- Synthesis and biological evaluation of novel imidazo[1,2-a]pyridine-oxadiazole hybrids as anti-proliferative agents: Study of microtubule polymerization inhibition and DNA binding
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Efforts towards the development of potential anticancer agents, a new series of imidazo[1,2-a]pyridine-oxadiazole hybrids were synthesized and evaluated for their in vitro anticancer activity against lung cancer (A549) and prostate cancer (PC-3, DU-145) cell lines. Amongst the compounds tested, 6d showed the highest potency on A549 cells with an IC50 value of 2.8 ± 0.02 μM. Flow cytometric analysis of compound 6d treated A549 cells showed apoptosis induction by annexin-v/PI dual staining assay and the effect of 6d on different phases of cell cycle was also analyzed. Target based studies demonstrated the inhibition of tubulin polymerization by 6d at an IC50 value of 3.45 ± 0.51 μM and its effective binding with CT-DNA. Further, the molecular modelling studies revealed that 6d has a prominent binding affinity towards α/β-tubulin receptor with admirable physico-chemical properties.
- Babu, Bathini Nagendra,Jadhav, Govinda Shivaji,Kadagathur, Manasa,Kiranmai, Gaddam,Nagesh, Narayana,Parimala Devi, G.,Sana, Sravani,Shankaraiah, Nagula,Sigalapalli, Dilep Kumar,Tangellamudi, Neelima D.,Tokala, Ramya,Tripura, Chaturvedula
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- Evaluation of the 2-substituent effect on the reactivity of the 8-haloimidazo[1,2-α]pyridine series towards Suzuki-type cross-coupling reaction
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The purpose of this work was to complete a general study that we initiated on the influence of a 2-substitution on the reactivity of 8-haloimidazo[1 ,2-α]pyridines towards a Suzuki cross-coupling reaction, using conventional reactants in order to obtain e
- Kazock, Jean-Yves,Enguehard-Gueiffier, Cecile,Thery, Isabelle,Gueiffier, Alain
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p. 154 - 159
(2007/10/03)
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