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Abstract Natural products remain a rich source of novel molecular scaffolds and neocryptolepine 1, and cryptolepine 2 an indoloquinoline alkaloid extracted from the roots of cryptolepis sanguinolenta are examples of natural products with wide biological activity. Besides their extraction from natural sources, several synthetic methodologies have been developed and novel neocryptolepine 1 and cryptolepine 2 derivatives with improved biological activity have been reported from our group and others. Prompted by these results, the main objective of this thesis work is to synthesize novel derivatives of the anticancer natural compound neocryptolepine 1 as part of a larger project of development of safer and potent anticancer drug candidates, at an affordable cost. The proposed approach is to synthesize neocryptolepine conjugates with an aminophosphonate 3, acridine 4 and rhodanine 5 surrogates, which are expected to improve the anticancer activity and the selectivity against cancer cells |