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Dive into the research topics where Anamik Shah is active.

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Featured researches published by Anamik Shah.


Bioorganic & Medicinal Chemistry | 2002

3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells.

Masami Kawase; Anamik Shah; Harsukh Gaveriya; Noboru Motohashi; Hiroshi Sakagami; Andreas Varga; Joseph Molnár

Fifteen 4-phenyl-3,5-dibenzoyl-1,4-dihydropyridines (BzDHPs) (1-15) substituted at the 4-phenyl ring were synthesized and compared to their cytotoxic activity and multidrug resistance (MDR)-reversing activity in in vitro assay systems. Among them, 2-CF3 (5) (IC50=8.7 microM), 2-Cl (11) (IC50=7.0 microM) and 3-Cl (12) (IC50=7.0 microM) derivatives showed the highest cytotoxic activity against human oral squamous carcinoma (HSC-2) cells. The activity of P-glycoprotein (Pgp) response for MDR in tumor cells was reduced by some of derivatives (3, 4, 8, 12), verapamil (VP) and nifedipine (NP). These data suggest that 3,5-dibenzoyl-4-(3-chlorophenyl)-1,4-dihydro-2,6-dimethylpyridine (12) can be recommended as a new drug candidate for MDR cancer treatment.


European Journal of Medicinal Chemistry | 2008

1,5-Benzothiazepine, a versatile pharmacophore: a review.

Jitender Bariwal; Kuldip Upadhyay; Atul Manvar; Jalpa Trivedi; Jyoti Singh; Kishor S. Jain; Anamik Shah

1,5-Benzothiazepine and 1,5-benzodiazipine are the two main seven-membered heterocyclic ring systems reported for their cardiac and psychotherapeutic activities. Successful introduction of diltiazem and clentiazem for angina pectoris, hypertension, arrhythmias and other related cardiac disorders proved potential of 1,5-benzothiazepine moiety. Subsequently 1,5-benzodiazepines were highlighted as important biologically active scaffolds. Also, discovery of thiazesim and quetiapine fumarate as psychotropic agents attracted much attention worldwide. The current review article focuses on pharmacological profile associated with 1,5-benzodiazepines. This article mainly covers structural modifications done for various targets along with the brief description of the targets.


Bioorganic & Medicinal Chemistry | 2001

SYNTHESIS AND QSAR STUDIES OF 4-SUBSTITUTED PHENYL-2,6-DIMETHYL-3,5-BIS-N-(SUBSTITUTED PHENYL) CARBAMOYL-1,4-DIHYDROPYRIDINES AS POTENTIAL ANTITUBERCULAR AGENTS

Bhavik Desai; Dinesh Sureja; Yogesh T. Naliapara; Anamik Shah; Anil K. Saxena

Synthesis and QSAR studies of the title compounds have resulted in the identification of structural and physicochemical parameters (MR, sigma(o), sigma(m), sigma(p)) contributing to antitubercular activity. Among these, carbamoyl phenyl ring substituted at 3 and 4 position with NO(2) group or 2 position with Cl or OCH(3) group shows >90% inhibition against H(37)Rnu comparable to other substituted phenyls.


Bioorganic & Medicinal Chemistry | 2008

Recent advances in selective α1-adrenoreceptor antagonists as antihypertensive agents

Kishor S. Jain; Jitender Bariwal; Muthu K. Kathiravan; Manisha S. Phoujdar; Rajkumari S. Sahne; Bishram Singh Chauhan; Anamik Shah; Mange Ram Yadav

Hypertension is one of the most serious health problems of the modern world with a continuous rise in the number of patients. Selective alpha(1)-adrenoreceptor antagonists though have many advantages and uses in the management of arterial hypertension, their lack of specificity at the level of alpha(1)-adr subtypes leads to multiple side effects. Existence of multiple alpha(1)-adr subtypes holds great promise for the discovery and development of more specific and selective drug molecules, targeting only one alpha(1)-adr subtype at a time and thus relative freedom from side effects. Herein, the research done on the discovery and evaluation of a variety of chemically diverse structures as selective antagonists of alpha(1)-adr and alpha(1)-adr subtypes in recent years has been reviewed.


European Journal of Medicinal Chemistry | 2008

Synthesis, anti-tubercular activity and 3D-QSAR study of coumarin-4-acetic acid benzylidene hydrazides

Atul Manvar; Alpeshkumar K. Malde; Jitender Verma; Vijay Virsodia; Arun Mishra; Kuldip Upadhyay; Hrishikesh Acharya; Evans C. Coutinho; Anamik Shah

A set of 25 coumarin-4-acetic acid benzylidene hydrazides were synthesized and characterized by NMR, IR and mass spectroscopic techniques. The compounds were evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H(37)Rv strain using the BACTEC 460 system to determine percentage inhibition. To understand the relationship between structure and activity, a 3D-QSAR analysis has been carried out by Comparative Molecular Field Analysis (CoMFA). Several statistically significant CoMFA models were generated. The CoMFA model generated with database alignment was the best in terms of overall statistics. The CoMFA contours provide a good insight into the structure activity relationships of the compounds reported herein.


Bioorganic & Medicinal Chemistry | 2011

Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates

Bhavin Marvania; Pei-Chih Lee; Ravi Chaniyara; Huajin Dong; Sharda Suman; Rajesh Kakadiya; Ting-Chao Chou; Te-Chang Lee; Anamik Shah; Tsann-Long Su

A series of N-mustard-quinazoline conjugates was synthesized and subjected to antitumor studies. The N-mustard pharmacophore was attached at the C-6 of the 4-anilinoquinazolines via a urea linker. To study the structure-activity relationships of these conjugates, various substituents were introduced to the C-4 anilino moiety. The preliminary antitumor studies revealed that these agents exhibited significant antitumor activity in inhibiting various human tumor cell growths in vitro. Compounds 21b, 21g, and 21h were selected for further antitumor activity evaluation against human breast carcinoma MX-1 and prostate PC-3 xenograft in animal model. These agents showed 54-75% tumor suppression with low toxicity (5-7% body-weight changes). We also demonstrate that the newly synthesized compounds are able to induce DNA cross-linking through alkaline agarose gel shift assay and inhibited cell cycle arrest at G2/M phase.


Bioorganic & Medicinal Chemistry Letters | 2011

Diversity oriented design of various hydrazides and their in vitro evaluation against Mycobacterium tuberculosis H37Rv strains

Atul Manvar; Abhay Bavishi; Ashish Radadiya; Jignesh Patel; Vipul Vora; Narshih Dodia; Kena Rawal; Anamik Shah

Control and prevention of tuberculosis is a major challenge, as one-third of the worlds population is infected with Mycobacterium tuberculosis. The resurgence of tuberculosis and the emergence of multidrug-resistance strains of mycobacteria, necessitate the search for new class of antimycobacterial agents. As a part of investigation of new antitubercular agents in this laboratory, we describe the syntheses of various hydrazides of comarins, quinolones and pyrroles and screening against M. tuberculosis (Mtb) H37(Rv) by using rifampin as a standard drug. Among the designed molecules, the most prominent compounds 2a-g, 4a and 9a showed >90% GI at MIC<6.25 μg/mL. Finally, these studies suggests that compounds 2a-g, 4a and 9a may serve as promising lead scaffolds for further generation of new anti-TB agents.


European Journal of Medicinal Chemistry | 2015

Bioactive benzofuran derivatives: An insight on lead developments, radioligands and advances of the last decade.

Ashish Radadiya; Anamik Shah

Benzofuran core is a highly versatile, presents in many important natural products and natural drugs. Many benzofuran containing synthetic drugs and clinical candidates have been derived from natural products. The present review will provide an insight on lead design-developments of the decade, clinical candidates and PET tracer radio-ligands containing benzofuran core along with brief target biology. Brief of the all approved drugs containing benzofuran core also have been enclosed. Main therapeutic areas covered are Cancer, Neurological disorders including anti-psychotic agent and diabetes.


Journal of Medicinal Chemistry | 2011

Structure-activity relationship of 4(5)-aryl-2-amino-1H-imidazoles, N1-substituted 2-aminoimidazoles and imidazo[1,2-a]pyrimidinium salts as inhibitors of biofilm formation by Salmonella typhimurium and Pseudomonas aeruginosa.

Hans Steenackers; Denis S. Ermolat’ev; Bharat Savaliya; Ami De Weerdt; David De Coster; Anamik Shah; Erik V. Van der Eycken; Dirk E. De Vos; Jozef Vanderleyden; Sigrid De Keersmaecker

A library of 112 4(5)-aryl-2-amino-1H-imidazoles, 4,5-diphenyl-2-amino-1H-imidazoles, and N1-substituted 4(5)-phenyl-2-aminoimidazoles was synthesized and tested for the antagonistic effect against biofilm formation by Salmonella Typhimurium and Pseudomonas aeruginosa. The substitution pattern of the 4(5)-phenyl group and the nature of the N1-substituent were found to have a major effect on the biofilm inhibitory activity. The most active compounds of this series were shown to inhibit the biofilm formation at low micromolar concentrations. Furthermore, the influence of 6 imidazo[1,2-a]pyrimidines and 18 imidazo[1,2-a]pyrimidinium salts on the biofilm formation was tested. These compounds are the chemical precursors of the 2-aminoimidazoles in our synthesis pathway. A good correlation was found between the activity of the imidazo[1,2-a]pyrimidinium salts and their corresponding 2-aminoimidazoles, supporting the hypothesis that the imidazo[1,2-a]pyrimidinium salts are possibly cleaved by cellular nucleophiles to form the active 2-aminoimidazoles. However, the imidazo[1,2-a]pyrimidines did not show any biofilm inhibitory activity, indicating that these molecules are not susceptible to in situ degradation to 2-aminoimidazoles. Finally, we demonstrated the lack of biofilm inhibitory activity of an array of 37 2N-substituted 2-aminopyrimidines, which are the chemical precursors of the imidazo[1,2-a]pyrimidinium salts in our synthesis pathway.


Bioorganic & Medicinal Chemistry Letters | 2011

Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT method.

Dhairya Bhavsar; Jalpa Trivedi; Shrey Parekh; Mahesh M. Savant; Shailesh Thakrar; Abhay Bavishi; Ashish Radadiya; Hardevsinh Vala; Jignesh Lunagariya; Manisha Parmar; Ladwa Paresh; Roberta Loddo; Anamik Shah

A series of novel N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives has been synthesized. All the newly synthesized compounds were evaluated for their anti-HIV activity using MTT method. Most of these compounds showed moderate to potent activity against wild-type HIV-1 with an EC(50) ranging from >7 EC(50) [μg/ml] to <100 EC(50) [μg/ml]. Among them, N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide 6v was identified as the most promising compound (EC(50)=<7 μg/ml). Among all the compounds, three compounds 6m, 6v and 6u have been exhibits potent anti-HIV activity against MT-4 cells.

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