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Chapter – 6 Biological evaluation of newly..... 6.3 IN SILICO STUDY FOR DNJ-701 In silico study for the indolinone derivatives, synthesized in Chapter – 3 (i.e. DNJ-701 to DNJ-705) and their anticancer activity was carried out at Gujarat Cancer Research Institute, (GCRI) Ahmedabad, which has been included in this chapter, while another coumarin derivatives synthesized in the same chapter are under investigation for their antitubercular and antiviral activity. Under this title, we are focusing on some advanced comparison data of molecule for possible risk assessment and for further development and conclusion. 1 – Toxicity Risk assessment 2 – logs Calculation 3 – Molecular Weight 4 – Drug likeness 5 – Drug Score O Cl N + N O - O Department of Chemistry, Saurashtra University, Rajkot – 360 005 339 Cl C30H18Cl2N4O3 N N
Chapter – 6 Biological evaluation of newly..... 6.3.1 TOXICITY RISK ASSESSMENT Recent high-profile drug withdrawals increase the pressure on regulators and the pharmaceutical industry to improve preclinical safety testing. Understanding mechanisms of drug toxicity is an essential step toward improving drug safety testing by providing the basis for mechanismbased risk assessments. Nonetheless, despite several decades of research on mechanisms of drug-induced toxicity and the application of various new technologies to preclinical safety assessment, the overall impact on preclinical safety testing has been modest. Assessing the risk of exposing humans to new drug candidates still depends on preclinical testing in animals, which in many, but not all cases, predicts outcomes in humans accurately. The following offers a perspective on the challenges and opportunities facing efforts to improve preclinical safety testing and outlines gaps and needs that must be addressed. A case is built for focusing solutions on defined problems within the current safety testing paradigm rather than imposing wholesale change. Targets for application of new technologies are available now. Improving drug safety testing will depend on improving the application of mechanism-based risk assessment but will also require improving public and private collaborations in order to focus research regarding the mechanism of drug-induced toxicity on the most important problems. Before doing the toxicity prediction we ran a set of toxic compounds and a set of presumably non-toxic compounds through the prediction. The data below shows the results obtained by predicting all available structures of four subsets of the database. E.g. all structures known to be mutagenic were run through the mutagenicity assessment. 86 % of these structures where found to bear a high or medium risk of being mutagenic. As a control set served a collection of traded drugs of which the mutagenicity risk assessment revealed only 12 % of potentially harmful compounds. Results of given substance, which obtain from one of those kind of procedures are mentioned. Department of Chemistry, Saurashtra University, Rajkot – 360 005 340
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Saurashtra University Re - Accredit
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Statement under O. Ph. D. 7 of Saur
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ACKNOWLEDGEMENT It is a moment of g
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Jignesh Lunagariya, Hitesh Sarvaiya
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CONTENT Content General Remarks 6 A
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Content 3.2 Reaction scheme 149 3.3
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5.14 Conclusion 313 5.15 Spectral r
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MF Molecular Formula MW Molecular W
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GABA Gamma Amino Butyric Acid MES M
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PART - A STUDIES ON 2-METHYL INDOLI
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Part-A Studies on 2-methyl indoline
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CHAPTER - 1 PREPARATION AND YIELD O
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Chapter - 1 Preparation and Yield o
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Part - B Studies on isatin derivati
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CHAPTER - 3 PREPARATION OF SMALL LI
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Chapter - 3 Preparation of small li
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CHAPTER - 4 STUDIES ON DIFFERENT TY
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Chapter - 4 Studies on different ty
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Chapter - 5 Synthesis and Character
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