- Synthesis and carbonic anhydrase I, II, VII, and IX inhibition studies with a series of benzo[d]thiazole-5- and 6-sulfonamides
-
A series of benzo[d]thiazole-5- and 6-sulfonamides has been synthesized and investigated for the inhibition of several human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms, using ethoxzolamide (EZA) as lead molecule. 2-Amino-substituted, 2-acylamino- an
- Abdoli, Morteza,Angeli, Andrea,Bozdag, Murat,Carta, Fabrizio,Kakanejadifard, Ali,Saeidian, Hamid,Supuran, Claudiu T.
-
-
Read Online
- Design, synthesis, and antipoliferative activities of novel substituted imidazole-thione linked benzotriazole derivatives
-
A new series of benzotriazole moiety bearing substituted imidazol-2-thiones at N1 has been designed, synthesized and evaluated for in vitro anticancer activity against the different cancer cell lines MCF-7(breast cancer), HL-60 (Human promyelocytic leukemia), and HCT-116 (colon cancer). Most of the benzotriazole analogues exhibited promising antiproliferative activity against tested cancer cell lines. Among all the synthesized compounds, BI9 showed potent activity against the cancer cell lines such as MCF-7, HL-60 and HCT-116 with IC50 3.57, 0.40 and 2.63 μM, respectively. Compound BI9 was taken up for elaborate biological studies and the HL-60 cells in the cell cycle were arrested in G2/M phase. Compound BI9 showed remarkable inhibition of tubulin polymerization with the colchicine binding site of tubulin. In addition, compound BI9 promoted apoptosis by regulating the expression of pro-apoptotic protein BAX and anti-apoptotic proteins Bcl-2. These results provide guidance for further rational development of potent tubulin polymerization inhibitors for the treatment of cancer.
- El-Malah, Afaf,Khayyat, Ahdab N.,Malebari, Azizah M.,Mohamed, Khaled O.
-
-
- Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II
-
Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells
- K?l?caslan, Soner,Arslan, Mustafa,Ruya, Zeynep,Bilen, ?igdem,Ergün, Adem,Gen?er, Nahit,Arslan, Oktay
-
p. 1300 - 1305
(2016/10/09)
-
- Inhibitors of apoptosis in testicular germ cells: Synthesis and biological evaluation of some novel IBTs bearing sulfonamide moiety
-
Pifithrin-α, a known p53 inactivator, inhibits p53-dependant mitochondrial cell death induced by toxins or γ-radiation. It has been found that aromatic IBT analogues of PFT-α are more cytoprotective and nonpeptide-based, isatin sulfonamides selectively in
- Chandak, Navneet,Bhardwaj, Jitender K.,Sharma, Rajnesh K.,Sharma, Pawan K.
-
p. 203 - 208
(2013/03/13)
-
- Heteroaromatic analogues of 1,5-diarylpyrazole class as anti-inflammatory agents
-
A novel series of heteroaromatic analogues of known anti-inflammatory (AI) drug celecoxib replacing the benzenesulfonamide moiety with 6- sulfonamidobenzothiazol-2-yl moiety was synthesized. Regioselective synthesis of the target compounds 2a-i having 1,5
- Sharma, Pawan K.,Chandna, Nisha,Kumar, Surender,Kmar, Pawan,Kumar, Satish,Kaushik, Pawan,Kaushik, Dhirender
-
p. 3757 - 3766
(2013/02/23)
-
- A library of novel allosteric inhibitors against fructose 1,6-bisphosphatase
-
The identification of a proper lead compound for fructose 1,6-bisphosphatase (FBPase) is a critical step in the process of developing novel therapeutics against type-2 diabetes. Herein, we have successfully generated a library of allosteric inhibitors against FBPase as potential anti-diabetic drugs, of which, the lead compound 1b was identified through utilizing a virtual high-throughput screening (vHTS) system, which we have developed. The thiazole-based core structure was synthesized via the condensation of α-bromo-ketones with thioureas and substituents on the two aryl rings were varied. 4c was found to inhibit pig kidney FBPase approximately fivefold better than 1b. In addition, we have also identified 10b, a tight binding fragment, which can be use for fragment-based drug design purposes.
- Heng, Sabrina,Gryncel, Kimberly R.,Kantrowitz, Evan R.
-
experimental part
p. 3916 - 3922
(2009/10/02)
-
- Synthesis and biological evaluations of sulfa derivatives bearing heterocyclic moieties.
-
Some new sulfa derivatives bearing a heterocyclic moieties fural, pyrimidinone, thiazolidinone, benzimidazole and 1,2,4-triazinone and the related compounds 2-19 have been synthesized from treatment of sulfa drugs with thioisocyanate, acid chlorides, 3-chloro-1,2,4-triazines, aldehydes, esters and/or 2-methylbenzoxazole followed by ring closure reactions. Structures of the products have been deduced from their elemental analysis and spectral data. Significant antimicrobial activities were observed in vitro for some members of the series. Compounds 9b, 16 are highly active, while compounds 4b, 6d, 7,9a, 10 and 14 showing a moderate active towards gramme positive bacterium (b.subtilis). gramme negative bacterium (E. coli) and two fungi namely (A.nidulans & A.terreus).
- Abdel-Monem, Wafaa R
-
p. 239 - 247
(2007/10/03)
-
- Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
-
Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
- -
-
Page column 56
(2008/06/13)
-
- CARBONIC ANHYDRASE INHIBITORS. PART 28. A NOVEL ROUTE TO SYMMETRICAL 2,5-DISUBSTITUTED-1,3,4-THIADIAZOLE DERIVATIVES VIA THIOUREAS
-
Reaction of sulfanilamide; 3,5-dichlorosulfanilamide; 5-amino-1,3,4-thiadiazole-2-sulfonamide and 5-imino-4-methyl-2-sulfonamido-δ2-1,3,4-thiadiazoline with potassium thiocyanate and HCl afforded the corresponding thioureas. these compounds wer
- Supuran, Claudiu T.
-
p. 643 - 652
(2007/10/03)
-