Synthesis of Novel Diaziridinyl Quinone Isoxazole Hybrids and Evaluation of Their Anti-Cancer Activity as Potential Tubulin-Targeting Agents
Two series of diaziridinyl quinone isoxazole derivatives were prepared and evaluated for their cytotoxic activity against MCF7, HeLa, BT549, A549 and HEK293 cell lines and interaction with tubulin. Compounds (6a-m) showed promising activity against all the 5 human cancer cell lines. Compounds 6a, 6e and 6 m were potent [IC 50 ranging between 2.21 μg to 2.87 μg] on ER-positive MCF7 cell line similar to the commercially available drug molecule Doxorubicin. The results from docking models are in consistent with the experimental values which demonstrated the favourable binding modes of compounds 6a-m to the interface of α- and β-tubulin dimer.
Kumar, P. Ravi,Yennam, Satyanarayana,Raghavulu,Velatooru, Loka Reddy,Kotla, Siva Reddy,Penugurti, Vasudevarao,Hota, Prasanta K.,Behera, Manoranjan,Jaya Shree
p. 406 - 414
(2019/07/10)
Synthesis of novel isoxazole-benzoquinone hybrids via 1,3-dipolar cycloaddition reaction as key step
An efficient method for the preparation of novel 2-(5-arylisoxazol-3-yl) cyclohexa-2,5-diene-1,4-dione hybrids via 1,3-dipolar cycloaddition followed by an oxidation reaction using ceric ammonium nitrate (CAN) has been described. Using this method, various aryl as well as alkyl substituted isoxazole-benzoquinone hybrids were synthesized in high yields.
Ravi Kumar,Behera, Manoranjan,Raghavulu,Jaya Shree,Yennam, Satyanarayana
p. 4108 - 4113
(2012/08/28)
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