Anticancer Potential of 3-(Arylideneamino)-2- Phenylquinazoline-4(3H)-One Derivatives
EPrints@IICB
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Title |
Anticancer Potential of 3-(Arylideneamino)-2- Phenylquinazoline-4(3H)-One Derivatives
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Creator |
Das, Subhadip
Chatterjee, Nabanita Bose, Dipayan Dey, Sumit Kr Munda, Rudra Narayan Nandy, Abhishek Bera, Sanjoy Biswas, Shyamal Kr Das Saha, Krishna |
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Subject |
Infectious Diseases and Immunology
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Description |
Different quinazoline derivatives have showed wide spectrum of pharmacological activities. Some 3- (arylideneamino)-phenylquinazoline-4(3H)-ones have been reported to possess antimicrobial activity. The present study has been undertaken to evaluate the anticancer effect of these quinazolinone derivatives. The quinazolinone derivatives were synthesized as reported earlier. Compounds containing NO2, OH, OCH3, or OH and OCH3 as substituent(s) on the arylideneamino group were named as P(3a), P(3b), P(3c), and P(3d) respectively. Out of these, P(3a) and P(3d) showed better cytotoxic activity than P(3b) and P(3c) on a panel of six cancer cell lines of different origin, namely, B16F10, MiaPaCa-2, HCT116, HeLa, MCF7, and HepG2, though the effect was higher in B16F10, HCT116, and MCF7 cells. P(3a) and P(3d) induced death of B16F10 and HCT116 cells was associated with characteristic apoptotic changes like cell shrinkage, nuclear condensation, DNA fragmentation, and annexin V binding. Also, cell cycle arrest at G1 phase, alteration of caspase-3, caspase- 9, Bcl-2 and PARP levels, loss of mitochondrial membrane potential, and enhanced level of cytosolic cytochrome c were observed in treated B16F10 cells. Treatment with multiple doses of P(3a) significantly increased the survival rate of B16F10 tumor bearing BALB/c mice by suppressing the volume of tumor while decreasing microvascular density and mitotic index of the tumor cells. |
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Publisher |
Karger
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Date |
2012
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Type |
Article
PeerReviewed |
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Format |
application/pdf
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Identifier |
http://www.eprints.iicb.res.in/1502/1/CELLULAR_PHYSIOLOGY_AND_BIOCHEMISTRY___29_(1%2D2)_251%2D260;2012[68].pdf
Das, Subhadip and Chatterjee, Nabanita and Bose, Dipayan and Dey, Sumit Kr and Munda, Rudra Narayan and Nandy, Abhishek and Bera, Sanjoy and Biswas, Shyamal Kr and Das Saha, Krishna (2012) Anticancer Potential of 3-(Arylideneamino)-2- Phenylquinazoline-4(3H)-One Derivatives. Cellular Physiology and Biochemistry, 29 (1-2). pp. 251-260. |
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Relation |
http://dx.doi.org/10.1159/000337606
http://www.eprints.iicb.res.in/1502/ |
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