Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones.

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Kamal A, Shaheer Malik M, Bajee S, Azeeza S, Faazil S, Ramakrishna S, Naidu VG, Vishnuwardhan MV

Synthesis and biological evaluation of conformationally flexible as well as restricted dimers of monastrol and related dihydropyrimidones.

Eur J Med Chem. 2011 Aug;46(8):3274-81. doi: 10.1016/j.ejmech.2011.04.048. Epub 2011 May 5.

PubMed ID

21620531 [ View in PubMed

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Abstract

A series of conformationally flexible and restricted dimers of monastrol as well as related dihydropyrimidones have been synthesized by employing one-pot Biginelli multicomponent reaction. These dimers have been evaluated for cytotoxic potency against selected human cancer cell lines and some of the compounds have exhibited more cytotoxic potency than the parent monastrol. Further, the DNA binding ability by thermal denaturation studies and antimicrobial activities of these compounds are also discussed.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Monastrol	Kinesin-like protein KIF11	IC 50 (nM)	14000	N/A	N/A	Details