716361-79-4Relevant academic research and scientific papers
Synthesis and evaluation of novel purple acid phosphatase inhibitors
Hussein, Waleed M.,Feder, Daniel,Schenk, Gerhard,Guddat, Luke W.,McGeary, Ross P.
, p. 61 - 71 (2019/01/30)
Transgenic studies in animals have demonstrated a direct association between the level of expression of purple acid phosphatase (PAP; also known as tartrate-resistant acid phosphatase) and the progression of osteoporosis. Consequently, PAP has emerged as
Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents
Prasad, Budaganaboyina,Lakshma Nayak,Srikanth,Baig, Mirza Feroz,Subba Reddy,Babu, Korrapati Suresh,Kamal, Ahmed
, p. 535 - 548 (2018/11/26)
A library of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides (7a–al) have been designed, synthesized and screened for their anti-proliferative activity against some selected human cancer cell lines namely DU-145, A-549, MCF-7 and HeLa. Most of them have shown promising cytotoxicity against lung cancer cell line (A549), amongst them 7f was found to be the most potent anti-proliferative congener. Furthermore, 7f exhibited comparable tubulin polymerization inhibition (IC50 value 2.04 μM) to the standard E7010 (IC50 value 2.15 μM). Moreover, flow cytometric analysis revealed that this compound induced apoptosis via cell cycle arrest at G2/M phase in A549 cells. Induction of apoptosis was further observed by examining the mitochondrial membrane potential and was also confirmed by Hoechst staining as well as Annexin V-FITC assays. Furthermore, molecular docking studies indicated that compound 7f binds to the colchicine binding site of the β-tubulin. Thus, 7f exhibits anti-proliferative properties by inhibiting the tubulin polymerization through the binding at the colchicine active site and by induction of apoptosis.
4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer
Reddy, V. Ganga,Bonam, Srinivasa Reddy,Reddy, T. Srinivasa,Akunuri, Ravikumar,Naidu,Nayak, V. Lakshma,Bhargava, Suresh K.,Kumar, H.M. Sampath,Srihari,Kamal, Ahmed
, p. 595 - 611 (2018/01/01)
Topoisomerases (topo-I and topo-II) have occupied a significant role in DNA replication, transcription, and are a promising set of antitumor targets. In the present approach, a series of new 4β-amidotriazole linked podophyllotoxin derivatives (10a-i and 1
Preparation method of 1-subtituted-1H-1,2,3-triazole-4-carboxylic acid
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Paragraph 0085; 0086; 0087; 0088, (2016/10/09)
The invention provides a preparation method of 1-subtituted-1H-1,2,3-triazole-4-carboxylic acid. The preparation method includes the following steps: 1-substituted-4,5-dibromo-1H-1,2,3-triazole is added to an isopropylmagnesium chloride, such that 1-substituted-4-bromo-1H-1,2,3-triazole is obtained through a reaction; an isopropylmagnesium chloride-lithium chloride complex is added directly, such that a mixture of 1-substituted-1H-1,2,3-triazole-4-carboxylic acid and 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylic acid is obtained; a base and iodomethane are added to the mixture, such that methyl 1-substituted-4-bromo-1H-1,2,3-triazole-5-carboxylare is obtained through a reaction; the aqueous layer is adjusted with hydrochloric acid until a pH value is 1-5; extraction is carried out with an organic solvent, and drying and concentration crystallization are carried out, such that 1-substituted-1H-1,2,3-triazole-4-carboxylic acid is obtained. The method is suitable for industrial production, and has a great application value.
Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands
Bai, Suping,Li, Shihong,Xu, Jinbin,Peng, Xin,Sai, Kiran,Chu, Wenhua,Tu, Zhude,Zeng, Chenbo,Mach, Robert H.
, p. 4239 - 4251 (2014/06/09)
Two novel classes of compounds targeting the sigma-2 (σ2) receptor were synthesized, and their bioactivities to binding σ1 and σ2 receptors were measured. Four novel triazole carboxamide analogues, 24d, 24e, 24f, and 39c, demonstrated high affinity and selectivity for the σ2 receptor. These data suggest 11C-labeled versions of these compounds may be potential σ2-selective radiotracers for imaging the proliferative status of solid tumors.
Triazole containing novobiocin and biphenyl amides as Hsp90 C-terminal inhibitors
Zhao, Jinbo,Zhao, Huiping,Hall, Jessica A.,Brown, Douglas,Brandes, Eileen,Bazzill, Joseph,Grogan, Patrick T.,Subramanian, Chitra,Vielhauer, George,Cohen, Mark S.,Blagg, Brian S. J.
supporting information, p. 1317 - 1323 (2014/10/15)
Hsp90 C-terminal inhibitors are advantageous for the development of new cancer chemotherapeutics due to their ability to segregate client protein degradation from induction of the prosurvival heat shock response, which is a major detriment associated with
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers
Kamal, Ahmed,Shaik, Bajee,Nayak, V. Lakshma,Nagaraju, Burri,Kapure, Jeevak Sopanrao,Shaheer Malik,Shaik, Thokhir Basha,Prasad
, p. 5155 - 5167 (2014/12/11)
A series of 1,2,3-triazole linked aminocombretastatin conjugates were synthesized and evaluated for cytotoxicity, inhibition of tubulin polymerization and apoptosis inducing ability. Most of the conjugates exhibited significant anticancer activity against
Inhibition of noroviruses by piperazine derivatives
Dou, Dengfeng,He, Guijia,Mandadapu, Sivakoteswara Rao,Aravapalli, Sridhar,Kim, Yunjeong,Chang, Kyeong-Ok,Groutas, William C.
supporting information; experimental part, p. 377 - 379 (2012/02/16)
There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize an array of structurally-diverse derivatives which were screened for anti-norovius activity in a cell-based replicon system. The studies described herein demonstrate for the first time that functionalized piperazine derivatives possess anti-norovirus activity. Furthermore, these studies have led to the identification of two promising compounds (6a and 9l) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics.
PYRAZOLE DERIVATIVES AS CYTOCHROME P450 INHIBITORS
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Page/Page column 82, (2008/06/13)
The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.
