- Synthesis, antiproliferative, and c-Src kinase inhibitory activities of 4-oxo-4H-1-benzopyran derivatives
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A new class of 4-oxo-4H-1-benzopyran derivatives were synthesized and their antiproliferative activity examined against a panel of three human cancer cell lines, that is, breast carcinoma (MDA-MB-468), ovarian adenocarcinoma (SK-OV-3), and colorectal adenocarcinoma (HT-29). Two compounds, that is, 3-hexyl-7,8-dihydroxy-4-oxo-4H-1-benzopyran and (E)-ethyl 3-(7-methoxy-4-oxo-4H-1-benzopyran-3-yl)acrylate were found to be potent against all three cancer cell lines studied at 50 μM concentration. Also, the inhibitory potency of the compounds was evaluated against active Src kinase. A few of these compounds exhibited modest Src kinase inhibitory activity (IC50 = 52-57 μM). Structure-activity relationship studies with respect to the nature and position of substituents on the lead compounds could be further exploited for the design and development of more potent antiproliferative agents and/or Src kinase inhibitors.
- Chand, Karam,Tiwari, Rakesh K.,Kumar, Sumit,Shirazi, Amir Nasrolahi,Sharma, Sweta,Van Der Eycken, Erik V.,Parmar, Virinder S.,Parang, Keykavous,Sharma, Sunil K.
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p. 562 - 572
(2015/03/30)
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- Inhibition of Alzheimer's BACE-1 by 2,6-dialkyl-4-chromon-3-yl-1,4-dihydropyridine-3,5-dicarboxylates
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Alzheimer's disease is the most common cause of dementia in the elderly, and no disease-modifying therapy is yet available for this devastating pathology. Deposition of different physicochemical forms of amyloid-β peptides is a critical phase in the patho
- Razzaghi-Asl, Nima,Aggarwal, Neha,Srivastava, Smriti,Parmar, Virinder S.,Prasad, Ashok K.,Miri, Ramin,Saso, Luciano,Firuzi, Omidreza
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p. 3230 - 3241
(2015/08/03)
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- Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives
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Src kinase, a prototype member of the Src family of kinases (SFKs), is over-expressed in various human tumors, and has become a target for anticancer drug design. In this perspective, a series of eighteen 2-pyridone derivatives were synthesized and evaluated for their c-Src kinase inhibitory activity. Among them, eight compounds exhibited c-Src kinase inhibitory activity with IC 50 value of less than 25 μM. Compound 1-[2-(dimethylamino)ethyl]- 5-(2-hydroxy-4-methoxybenzoyl)pyridin-2(1H)-one (36) exhibited the highest c-Src kinase inhibition with an IC50 value of 12.5 μM. Furthermore, the kinase inhibitory activity of compound 36 was studied against EGFR, MAPK and PDK, however no significant activity was observed at the highest tested concentration (300 μM). These results provide insights for further optimization of this scaffold for designing the next generation of 2-pyridone derivatives as candidate Src kinase inhibitors.
- Chand, Karam,Prasad, Suchita,Tiwari, Rakesh K.,Shirazi, Amir N.,Kumar, Sumit,Parang, Keykavous,Sharma, Sunil K.
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- Derivatives of 1,3,5-Triazine: Part III - Cyanuric Chloride-Dimethylformamide as a New Reagent for Synthesis of Amides, Esters, Aldehydes and for Dehydration Reactions
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Cyanuric chloride reacts with dimethylformamide to form a complex (I), which can be used directly for the synthesis of amides, esters, relatively simple peptides, aldehydes and for dehydration reactions.
- Lahoti, R. J.,Wagle, D. R.
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p. 1007 - 1008
(2007/10/02)
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- Chromonealdehyde compounds and process for the production thereof
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There are provided compounds of the general formula SPC1 Wherein R is a hydroxy, alkyl, acyloxy, halogen, nitro, substituted or unsubstituted amino, alkoxy, carboxy or a group derived from a carboxy group and m is 0, 1 or 2 except where m is 2, the two R groups are both hydroxy groups. The present invention is also concerned with a process for preparing the chromonealdehyde compounds. The chromonealdehyde compounds are characterized by antiallergic properties and are therefore useful as prophylactic and therapeutic agents for allergic asthma, allergic dermatitis and other allergic diseases and also are valuable as intermediates for the synthesis of other pharmaceutical compounds having the chromone nucleus.
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