Amphiphilic Indole Derivatives as Antimycobacterial Agents: Structure–Activity Relationships and Membrane Targeting Properties

2017 ◽  
Vol 60 (7) ◽  
pp. 2745-2763 ◽  
Author(s):  
Tianming Yang ◽  
Wilfried Moreira ◽  
Samuel Agyei Nyantakyi ◽  
Huan Chen ◽  
Dinah binte Aziz ◽  
...  
Keyword(s):  
Membrane Targeting ◽  
Indole Derivatives ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Antimycobacterial Agents

Improved synthesis of 4-/6-substituted 2-carboxy-1H-indole-3-propionic acid derivatives and structure–activity relationships as GPR17 agonists

MedChemComm ◽  
2014 ◽  
Vol 5 (1) ◽  
pp. 86-92 ◽  
Author(s):  
Younis Baqi ◽  
Samer Alshaibani ◽  
Kirsten Ritter ◽  
Aliaa Abdelrahman ◽  
Andreas Spinrath ◽  
...  
Keyword(s):  
Propionic Acid ◽  
Indole Derivatives ◽  
Structure Activity Relationships ◽  
Structure Activity

Several tri- and tetra-substituted indole derivatives were synthesized and evaluated as human GPR17 agonists. Steep structure–activity relationships were observed.

Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives

1993 ◽  
Vol 36 (8) ◽  
pp. 1053-1068 ◽  
Author(s):  
Chiu Hong Lin ◽  
Susanne R. Haadsma-Svensson ◽  
Robert A. Lahti ◽  
Robert B. McCall ◽  
Montford F. Piercey ◽  
...  
Keyword(s):  
Indole Derivatives ◽  
Structure Activity Relationships ◽  
Dopaminergic Agents ◽  
Structure Activity

Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives

1993 ◽  
Vol 36 (8) ◽  
pp. 1069-1083 ◽  
Author(s):  
Chiu Hong Lin ◽  
Susanne R. Haadsma-Svensson ◽  
Gillian Phillips ◽  
Robert A. Lahti ◽  
Robert B. McCall ◽  
...  
Keyword(s):  
Indole Derivatives ◽  
Structure Activity Relationships ◽  
Dopaminergic Agents ◽  
Structure Activity

Indole derivatives (2010–2020) as versatile tubulin inhibitors: synthesis and structure–activity relationships

2021 ◽  
Vol 13 (20) ◽  
pp. 1795-1828
Author(s):  
Fatima Naaz ◽  
Kumari Neha ◽  
Md Rafi Haider ◽  
Syed Shafi
Keyword(s):  
Cancer Therapy ◽  
Present Article ◽  
Dynamic Equilibrium ◽  
Biological Activities ◽  
Indole Derivatives ◽  
Tubulin Inhibitors ◽  
Structure Activity Relationships ◽  
Drug Candidates ◽  
Structure Activity ◽  
Wide Range

Tubulin inhibitors are conjugates that interfere with the dynamic equilibrium of the polymerization and depolymerization of microtubules. Among all the reported conjugates, indole moiety is one of the most significant classes for the development of new drug candidates for cancer therapy. Due to their presence in a wide range of natural as well as synthetic antitubulin agents, indole has become a versatile scaffold in research, and various synthetic and semisynthetic indole-based antitubulin agents have been identified and reported. The present article focuses on the reported indole-based tubulin inhibitors of synthetic origin from last the decade. Synthesis, structure–activity relationships and biological activities of synthetic indole derivatives along with brief updates on their antitubulin activity are presented.

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