Synthesis And Anti-proliferation Activity Evaluation Of Novel Dehydroepiandrosterone D-ring Fused Heterocyclic Analogues

Steroidal compounds are widely existent in the natural world and display avariety of biological activities, expecially the modification on the cycles of A and D.Meanwhile thiazole is a ubiquitous building block in medicinal chemistry and can befound in numerous natural products. Nitrogen-containing fused heterocyclesconstitute important core fragments in natural products and pharmaceutical agents,imparting unique physical and biological properties. The synthesis of heterocycliccompounds containing chromeno thiazole motifs has gained importance due to theirwidespread usage in the treatment of impulsive disorders, Parkinson’s disease,psychoses, memory disorders. The highlights of my research work are as follows:1. A series of steroidal[17,16-d]thiazole were synthesized through a convenientand productive method by using Dehydroepiandrosterone as the starting material.Through condensation of Dehydroepiandrosterone and thiourea we got the targetcompounds. The pure form of these compounds were achieved by crystallization.2. A series of steroidal[17,16-d]thiazole, steroidal[1,2-b]pyridine and steroidal[17,16-d]thiazole[2,1-b]imidazo products were synthesized through a convenient andproductive method. The in vitro antiprolifration evaluation results showed that most ofthis series possess a good activity against EC109(human esophageal carcinoma),EC9706(human esophageal carcinoma) and MGC-803(human gastric carcinoma)cell lines.3. All the compounds reported here are first synthesized and the structures arealso confirmed by NMR and MS spectras.