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Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C‐43 semi‐synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs in the clinic. Following our previous research on antitumor rapalogs modified on the C‐43 position, 13 novel rapamycin triazole hybrids (6a–g, 7a–f...
Rapamycin, a potent antifungal antibiotic, was approved as immunosuppressant, and lately its derivatives have been developed into mTOR targeting anticancer drugs. Structure modification was performed at the C‐42 position of rapamycin, and a novel series of rapamycin triazole hybrids (4a–d, 5a–e, 8a–e, and 9a–e) was facilely synthesized via Huisgen's reaction. The anticancer activity of these compounds...
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