応用薬学ジャーナル
オープンアクセス

概要

CAMPTOTHECIN AND ITS ANALOGS ANTITUMOR ACTIVITY BY POISONING TOPOISOMERASE I, THEIR STRUCTUREACTIVITYRELATIONSHIPANDCLINICALDEVELOPMENT PERSPECTIVEOFANALOGS

Muqeet Wahid, Qudsia Bano

Camptothecin or CPT and its analogs appear to employ anticancer action by poisoning topoisomerase I (topo I) enzyme. As a result topo I activity inhibited and have established important role against a wide range of tumors. CPT was extracted from bark of Chinese plant Camptotheca acuminate but now a large number of synthetic and semi-synthetics are identified. After activity, researchers organized evaluation of A, B and E-ring modified CPT reported analogs. This review illustrated a discussion of modern approaches in medicinal chemistry development of CPT, effective anticancer agent that targets topoisomerase I and also with their Clinical studies. This review summarizes the mode of action of CPT, the structure-activity relationship (SAR), a list of CPT analogs and their biological action with detail clinical development.