3 years ago

The uses of cyclohexan-1,4-dione for the synthesis of thiophene derivatives as new anti-proliferative, prostate anticancer, c-Met and tyrosine kinase inhibitors

Rehab A. Ibrahim, Rafat M. Mohareb, Fatima Al-Omran


A series of heterocyclic compounds derived from the dihydrobenzo[b]thiophene derivatives were synthesized all the synthesized compounds were determined by elemental analysis, 1H NMR, 13C NMR, and MS. The newly synthesized compounds were evaluated for their in-vitro cytotoxic activity against c-Met kinase, and the six typical cancer cell lines (A549, H460, HT-29, MKN-45, U87MG, and SMMC-7721). All target compounds were initially tested for their anti-proliferative activity against human prostatic cancer PC-3 cell line. The most promising compounds were 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 7b, 7c, 11c, 11d, and 11f were further investigated against tyrosin kinase (c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR). Compounds 5e, 5f, 5h, 11d, and 11f were selected to examine their Pim-1 kinase inhibition activity where compounds 5e, 5h, and 11f showed high activities.

Publisher URL: https://link.springer.com/article/10.1007/s00044-017-2087-3

DOI: 10.1007/s00044-017-2087-3

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