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ANNUAL REPORT Kunming Institute of Botany, Chinese Academy ...

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<strong>Kunming</strong> <strong>Institute</strong> <strong>of</strong> <strong>Botany</strong>, <strong>Chinese</strong> <strong>Academy</strong> <strong>of</strong> SciencesAnnual ReportA Series <strong>of</strong> Platinum Complexes Exhibit SelectiveCytotoxicity towards Cancer CellsPlatinum-based drugs have become fundamentalcomponents <strong>of</strong> standard chemotherapy regiments,and are widely used in antitumor therapy <strong>of</strong> testicularand ovarian tumors, lung and colorectal carcinomas.Despite the therapeutic benefit, the efficacy <strong>of</strong>platinum-based treatment regiments is considerablycompromised not only by severe side-effects but alsoby insurmountable cross-resistance.With coorperation between Pr<strong>of</strong>. LIU Wei-Ping'sgroup in <strong>Kunming</strong> <strong>Institute</strong> <strong>of</strong> Precious Metals, andPr<strong>of</strong>. LI Yan's group in KIB, a series <strong>of</strong> platinum (II)complexes were designed and synthesized featuringa dichloroactetate moiety tethered to the leavinggroup via ester bond, Among <strong>of</strong> which, mixed-NH3/cyclopentamine platinum(II) complexes <strong>of</strong>3-dichoroacetoxylcyclobutane-1,1-dicarboxylateexhibit selective cytotoxicity towards cancer cellsthrough inducing the apoptosis <strong>of</strong> cancer cells,whereas leaving the normal cells much less affected.Also, the complexes are able to overcome theresistance <strong>of</strong> cancer cells to cisplatin, which show apromising value for further exploration. The patenton the structures and activities has been authorized(ZL20101027465.2).The structures <strong>of</strong> synthesized complexesTable1. selective cytotoxicity <strong>of</strong> synthesized complexes towards cancer cells [a]IC50 (μM)complexSK-OV-3 SGC-7901 22RV-1 A549 Beas-2BSIKK-01 46.7 56.1 58.9 61.8 79.9 1.29KK-04 43.3 31.4 25.9 50.9 59.8 1.17KK-05 18.8 22.1 17.1 17.1 60.1 3.51KK-06 10.6 16.8 18.2 15.2 52.3 3.44Cisplatin 7.15 13.7 13.2 14.8 11.6 0.78Carboplatin 100 127 64.8 140 73.7 0.52 —— HIGHLIGHTS OF ACHIEVEMENTS ——

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