Design and Development of Small-Molecule Arylaldoxime/5-Nitroimidazole Hybrids as Potent Inhibitors of MARK4: a Promising Approach for Target-Based Cancer Therapy

Autor: Imtaiyaz Hassan, Amir Azam, Fernando Avecilla, Shadab Miyan Siddiqui, Nashrah Sharif Khan, Parvez Khan, Mudasir Nabi Peerzada

Publikováno v: ACS Omega, Vol 5, Iss 36, Pp 22759-22771 (2020)
RUC. Repositorio da Universidade da Coruña
Universitat Oberta de Catalunya (UOC)
RUC: Repositorio da Universidade da Coruña
Universidade da Coruña (UDC)
ACS Omega

[Abstract] Microtubule affinity-regulating kinase 4 (MARK4), a member of the serine/threonine kinase family, is an emerging therapeutic target in anticancer drug discovery paradigm due to its involvement in regulation of microtubule dynamics, cell cy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a643d55ed233cfe43aba6f24f54b31ce
https://hdl.handle.net/2183/26590

Metronidazole hydrazone conjugates: Design, synthesis, antiamoebic and molecular docking studies

Autor: Neelima Mondal, Shadab Miyan Siddiqui, Subhash Mohan Agarwal, Mohammad Fawad Ansari, Amir Azam, Kunwar Somesh Vikramdeo

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:3545-3549

Metronidazole hydrazone conjugates (2-13) were synthesized and screened in vitro for antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Six compounds were found to be better inhibitors of E. histolytica than the reference drug me

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a87ff2894784115b311b1567119987c
https://doi.org/10.1016/j.bmcl.2015.06.091

Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents

Autor: Shadab Miyan Siddiqui, Afreen Inam, Ana Cristina Lima Leite, Amir Azam, Milena Botelho Pereira Soares, Taís S. Macedo, Diogo Rodrigo Magalhães Moreira

Publikováno v: European Journal of Medicinal Chemistry. 75:67-76

N-Acylhydrazones derived from 7-chloro-4-piperazin-1-yl-quinoline were synthesized and biologically evaluated for blood-stage of Plasmodium falciparum and Entamoeba histolytica trophozoites. N-Acylhydrazone F12 was found to inhibit the P. falciparum

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1db96621dcf5f153e032733198e3d6ee
https://doi.org/10.1016/j.ejmech.2014.01.023

Synthesis of some 1,3,4-thiadiazole derivatives as inhibitors of Entamoeba histolytica

Autor: Shadab Miyan Siddiqui, Amir Azam, Attar Salahuddin

Publikováno v: Medicinal Chemistry Research. 22:1305-1312

In the quest for potent anti-amoebic agents, some 1,3,4-thiadiazole derivatives were synthesized and characterized by spectral data. The purity of the compounds was confirmed by elemental analysis. All the compounds were screened in vitro against HM1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::35163ad024240b79896b807817a07d60
https://doi.org/10.1007/s00044-012-0107-x

Pyrazolo[3,4-d]pyrimidine analogues: synthesis, characterization and their in vitro antiamoebic activity

Autor: Shadab Miyan Siddiqui, Attar Salahuddin, Amir Azam

Publikováno v: Medicinal Chemistry Research. 22:775-781

Pyrazolo[3,4-d]pyrimidine analogues were synthesized by treating 3-phenyl-1H-pyrazolo[3,4-d]pyrimidine-4-amine with different sulfonyl chlorides and triethylamine in dry dichloromethane. The structure of all the compounds was elucidated by spectral d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e014451d90cb02be4601ef1760910bd6
https://doi.org/10.1007/s00044-012-0070-6