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Part-IIIResults and DiscussionVIIxxviCl4 R123 565,01 225,60 7,95 1,21 7VIIxxviiO4 R123 567,04 221,23 24,17 3,68 11VIIxxviiiOOO4 R123 564,75 222,69 6,11 0,93 5VIIxxixVIIxxxOH4 R123 568,09 225,82 6,78 1,03 64 R123 571,58 222,31 6,39 0,97 5FAR: Fluorescence Activity RatioDMSO control 20 µl R123 580,10 226,24 6,52 0,99 5MDR - R123 574,51 239,73 6,19 - 5470
3.5 DiscussionPart-IIIResults and DiscussionIn the present report, hybrid derivatives (thio and oxo analogues) of DP-7(dihydropyridine) and monastrol (dihydropyrimidines) were synthesized to get the dualaction in cancer chemotherapy. The newly synthesized molecules were screened onMDR1-gene transfected mouse lymphoma cell line (l5178 y) for MDR reversal effects atnon toxic concentrations.MDR reversal assay has gained importance in view of many cancerous cells developingmultiple drug resistance (MDR) due to incorporation of MDR-1 gene coding of Pgp, aglycoprotein involved in MDR. The glycoprotein Pgp is driven by ATP and is responsiblefor efflux of drug from the cancerous cells leading to MDR. Therefore, MDR reversalagents are being exploited as potential anticancer agents. 9-10The four compounds from this series were very effective, namely 5-benzoyl-6-methyl-4-(1-naphthyl)-3,4-dihydropyrimidin-2(1H)-one (VIIvii), 4-(2,5-dimethoxyphenyl)-6-methyl-5-(1-phenylvinyl)-3,4-dihydropyrimidin-2(1H)-one (VIIix), 5-benzoyl-4-(3Hindol-3-yl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one(VIIx) and [6-methyl-4-(3-phenoxyphenyl)-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl](phenyl)methanone(VIIxxvii) when measured in 4 micromol/ml/1million cells. These compounds hadmoderate effect on the MDR reversal efflux pump activity.The substitution of 3-phenyloxy ring on 4 th phenyl ring in case of (VIIviii) resulted anineffective compounds while dimethoxy, indolyl and napthyl substituents are very activeas resistance modifiers The differences in biological effects can be explained by stericdifferences in binding abilities of compounds to Pgp. Direct evidence of the nature ofeffective binding of the four most effective compounds to Pgp could be obtained by X-raydiffraction of co-crystallizations.471
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Saurashtra UniversityRe - Accredite
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Statement Under O.Ph.D. 7 of Sauras
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ContentsAcknowledgementRegistration
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Contents1.2 Synthesis of condensed
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Contents1.5 MDR modulators 3981.6 D
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infrastructure and all the faciliti
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Above all I thank Lord Hanuman Ji a
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Abbreviations used1 H NMR Proton Nu
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UVVEGFRWCRWHOZ-EUltra VioletVascula
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22. 2-Substitutedthieno[3,2-d]/benz
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PrefacePrefaceHeterocyclic chemistr
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PrefaceThis entire cascade of react
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PrefaceOONHNHPOCl 3MWINVi-xviiClClC
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PrefaceOOHOOOONHNHDP-7 1NHMonastrol
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PART-I
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3.7 Results and discussion on biolo
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Part-1Review on Antiulcer Literatur
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Table 2: Distinguishing Features of
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1.2.2. Muscarinic AntagonistsPart-1
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1.5.5. Pharmacological PropertiesPa
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2. Aim of the Present WorkPart-IAim
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Part-IAim of Present WorkR 2 OR 3 R
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2.2. Bacisity of Pyridine vs Pyrimi
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Part-IAim of Present WorkOANNHOSNHN
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Part-IAim of Present WorkS. No. A S
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3. Results and Discussion
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Part-IResults and Discussion3.1.1d
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Part-IResults and DiscussionOR 1XR
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Part-IResults and Discussionformed
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Part-IResults and DiscussionOOON 2
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c. Synthesis of 2-carbethoxy-3-amin
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Part-IResults and DiscussionTable 7
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Part-IResults and DiscussionOOEtNHO
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Part-IResults and DiscussionTable-8
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Part-IResults and DiscussionCompd.N
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Part-IResults and DiscussionStep-IY
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S. No. Y Mol. Formula(Sol. ofrecrys
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Part-IResults and DiscussionS. No.
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Part-IResults and DiscussionONNHIII
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Part-IResults and DiscussionS. No.A
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Part-IResults and Discussion3.5. Sp
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Specimen 1 H NMR spectra of 2-chlor
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Part-IResults and Discussioninvolve
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Part-IResults and DiscussionSpecime
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The Infrared (IR) spectra:Part-IRes
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Part-IResults and DiscussionR 1ON+
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Part-IResults and DiscussionOSNHOSN
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3.6 Biological Evaluation of PPI’
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Part-IResults and DiscussionExperim
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Part-IResults and DiscussionDrug Pr
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Table 11. Effect of newly synthesiz
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Part-IResults and DiscussionS.No.AR
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Part-IResults and DiscussionS.No.AR
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Figure-1. Effect of newly synthesiz
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Figure-3. Effect of newly synthesiz
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Part-IResults and DiscussionFigure
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Part-IResults and DiscussionFigure
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Part-IResults and Discussion2. Effe
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Part-IResults and Discussionby kine
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Part-IResults and DiscussionNNNNNHN
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3.8. QSAR StudiesPart-IResults and
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Part-IResults and DiscussionFigure-
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Part-IResults and DiscussionPhysico
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Part-IResults and DiscussionThe MDS
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2. Volume of gastric secretion:Desc
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Part-IResults and DiscussionFor the
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3. Ulcer scoreDescription of the de
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Part-IResults and Discussion24. Ros
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4. Experimental
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Part-IExperimental119 o C was 128-1
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5. Synthesis of ethyl 2-amino-4-phe
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Part-IExperimentalthe procedure des
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Part-IExperimentalRecrystallization
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Part-IExperimentalM.P. : 132-134 o
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Part-IExperimentalA solution of thi
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Part-IExperimentalNMR (CDCl 3 )δpp
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Part-IExperimental6. Reaction of et
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Part-IExperimentalNMR (CDCl 3 )δpp
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Part-IExperimentalM.P. : 240-245 o
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Part-IExperimentalrecrystallization
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Part-IExperimental(1H, d, CH at imi
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Part-IExperimentalNMR (DMSO-d 6 )δ
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M.P. : 140-142 o C; Yield: 73%.Mol.
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M.P. : 135-141 o C; Yield: 67%.Mol.
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Part-IExperimentalml), over a perio
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Part-IExperimentalchloride was adde
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Part-IExperimental29. Synthesis of
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Part-IExperimentalIR (KBr) cm -1 :
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Part-IExperimentaladded while stirr
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Part-IExperimentald]pyrimidin-4(3H)
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Part-IExperimentalMol. formula : C
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Part-IExperimentalthis clear soluti
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Part-IExperimentalwhile maintaining
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Part-IExperimentalMol. Formula : C
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PART-II
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Part-IIContents2.3.2.1 Mononuclear
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Part-IISynthesis of Pyrimidines1. S
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Part-IISynthesis of PyrimidinesYZR
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Part-IISynthesis of Pyrimidineselec
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Part-IISynthesis of PyrimidinesR 1R
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Part-IISynthesis of Pyrimidinespyri
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R 1 R 2 R Yield(%)Part-IISynthesis
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Part-IISynthesis of Pyrimidinesyiel
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Table 27: 2-Amino-3-substitutedaryl
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Part-IISynthesis of PyrimidinesWhil
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Part-IISynthesis of PyrimidinesSimi
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Part-IISynthesis of PyrimidinesTabl
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R 1 R 2 R X Yield(%)Part-IISynthesi
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Part-IISynthesis of Pyrimidines+RCN
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Part-IISynthesis of PyrimidinesNN+
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Part-IISynthesis of PyrimidinesR 1+
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Part-IISynthesis of Pyrimidinesthe
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Part-IISynthesis of Pyrimidinesacet
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Part-IISynthesis of Pyrimidinesexpe
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Part-IISynthesis of PyrimidinesNOOC
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Part-IISynthesis of PyrimidinesThe
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Part-IISynthesis of PyrimidinesTabl
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Part-IISynthesis of PyrimidinesOH 3
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1.10 ReferencesPart-IISynthesis of
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Part-IISynthesis of Pyrimidines42.
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2. Impact of Microwave Assisted Hea
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Part-IIImpact of Microwave…Microw
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Part-IIImpact of Microwave…Figure
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Part-IIImpact of Microwave…R 1ArR
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Part-IIImpact of Microwave…as an
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Part-IIImpact of Microwave…al. 21
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Part-IIImpact of Microwave…XOHR 1
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Part-IIImpact of Microwave…N+N21B
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Part-IIImpact of Microwave…OO+ NO
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Part-IIImpact of Microwave…NO 2NO
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Part-IIImpact of Microwave…RNHNNH
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Part-IIImpact of Microwave…assist
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Part-IIImpact of Microwave…CNRNH
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Part-IIImpact of Microwave…Multig
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Part-IIImpact of Microwave…Nie et
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Part-IIImpact of Microwave…synthe
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Part-IIImpact of Microwave…An eff
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Part-IIImpact of Microwave…OO+S 8
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2.6. ReferencesPart-IIImpact of Mic
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49. Baxendale, I. R.; Ley, S. V. J.
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Part-IIAim of the Present Work3. Ai
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Part-IIAim of the Present WorkONHR
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Part-IIAim of the Present WorkYZXNN
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Part-IIAim of the Present WorkThe c
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3.5 References:Part-IIAim of the Pr
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Part-IIAim of the Present Work37. S
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Part-IIResults and Discussion4.1 Sy
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4.2 Synthesis of condensed 2-substi
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Table 38: Physical data of condense
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S. No. X Time ofMWIHeating(Min)VxiV
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S. No. X Time ofMWIHeating(Min)Yiel
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4.3 Synthesis of condensed 4-chloro
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Part-IIResults and DiscussionHerein
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Part-IIResults and DiscussionS. No.
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Part-IIResults and DiscussionS. No.
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The Mass spectraPart-IIResults and
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Specimen IR spectra of some 2-chlor
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Part-IIResults and Discussion1 H NM
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Part-IIResults and Discussionion (c
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Specimen 1 H NMR spectra of 4-chlor
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Part-IIResults and Discussion4.5 MD
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Part-IIResults and DiscussionH 3CO1
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Part-IIResults and DiscussionCl14.
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Part-IIResults and DiscussionO14. V
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4.6 References:Part-IIResults and D
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5. ExperimentalPart-IIExperimentalA
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3. Synthesis of 2-chloromethyl-5-ph
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Part-IIExperimentalIR (KBr) cm -1 :
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Part-IIExperimentalM.P. : 247-249 o
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Part-IIExperimental5.4 Synthesis of
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Part-IIExperimentalwere reacted und
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27. Synthesis of 2-methyl-5-phenylt
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Part-IIExperimental80 o C) that yie
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Part-IIExperimental36. Synthesis of
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Part-IIExperimentalunder microwave
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Part-IIExperimentalM.P. : >300 o C
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M.P. : 280-282 o C; Yield: 90%Mol.
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5.10 References:Part-IIExperimental
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Synthesis, Characterization and Ant
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Part-IIIAdvances Dihydropyridines a
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CH 3CH 3Part-IIIAdvances Dihydropyr
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Page 467 and 468: Part-IIIAdvances Dihydropyridines a
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Page 501 and 502: 3. Results and Discussion
Page 503 and 504: Part-IIIResults and DiscussionOOOHR
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Page 507 and 508: Part-IIIResults and DiscussionS. No
Page 509 and 510: S. No R X MolFormula(Sol. of Recrys
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Page 513 and 514: Specimen 13 C NMR spectra of some D
Page 515 and 516: Part-IIIResults and DiscussionTable
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Page 521 and 522: 4. Experimental
Page 523 and 524: Part-IIIExperimentalglacial acetic
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Page 537 and 538: Summary and Conclusion
Page 539 and 540: Summary and Conclusionactivity in P
Page 541 and 542: Summary and Conclusionreverting act
Page 543 and 544: Publications and Presentations
Page 545 and 546: Publications and PresentationsOther
Page 547: Publications and Presentations8. K.
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