A Facile Regioselective Synthesis of New Class of Cyclopent[b]indole dispiro heterocycles via1,3-Dipolar Cycloaddition protocol and invitro Cytotoxic studies

作者：Satheeshkumar Rajendran; Edatt Lincy; Kumar V B Sameer; Prasad Karnam Jayarampillai Rajendra^*

来源：ChemistrySelect, 2017, 2(9): 2626-2633.

DOI：10.1002/slct.201700157

• 1,3-Dipolar cycloaddition
• Azomethine ylides
• Cyclopent[b]indole dispiro heterocycles
• HeLa and MCF-7
• SAR studies

The construction of azomethine ylides insitu from acenaphthoquinone/isatin and secondary amino acids such as sarcosine and thiaproline with cyclopent[b]indole dipolarophilesin refluxing dioxane and methanol afforded novel class of cyclopent[b]indole dispiro heterocycles via 1,3-dipolar cycloaddition reaction. The regio and stereochemistry of formation of the final product was concertedly assigned by proton, carbon and 2DNMR techniques. Among the synthesized dispiroheterocyclic compounds 4&7 are found to show better cytotoxic activity against HeLa and MCF-7 with structure activity relationship (SAR) studies.

• 出版日期2017-3-23