Design and synthesis of herboxidiene derivatives that potently inhibit in vitro splicing

2021 ◽  
Vol 19 (6) ◽  
pp. 1365-1377
Author(s):  
Arun K. Ghosh ◽  
Srinivasa Rao Allu ◽  
Guddeti Chandrashekar Reddy ◽  
Adriana Gamboa Lopez ◽  
Patricia Mendez ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design And Synthesis ◽  
In Vitro Splicing ◽  
Enantioselective Syntheses ◽  
Derivatives Of

Enantioselective syntheses of C-6 modified derivatives of herboxidiene and their biological evaluation in splicing inhibitory assay.

scholarly journals Design, synthesis and in vitro splicing inhibition of desmethyl and carba-derivatives of herboxidiene

2016 ◽  
Vol 14 (23) ◽  
pp. 5263-5271 ◽  
Author(s):  
Arun K. Ghosh ◽  
Kai Lv ◽  
Nianchun Ma ◽  
Emilio L. Cárdenas ◽  
Kerstin A. Effenberger ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
In Vitro Splicing ◽  
Enantioselective Syntheses ◽  
Derivatives Of

Enantioselective syntheses of the desmethyl and carba-derivatives of herboxidiene and their biological evaluation in splicing assay are reported.

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

scholarly journals Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors

2013 ◽  
Vol 7 (1) ◽  
pp. 39-48 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Ghassan Abu Sheikha ◽  
Mahmoud Al-Sha'er ◽  
Mutasem Taha
Keyword(s):  
Acetic Acid ◽  
Type Ii Diabetes Mellitus ◽  
Biological Evaluation ◽  
Diabetic Patients ◽  
Type Ii ◽  
Design Synthesis ◽  
Multifunctional Protein ◽  
Design And Synthesis ◽  
Dpp Iv

As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein involved in many physiological processes. It deactivates the natural hypoglycemic incretin hormone effect. Inhibition of this enzyme increases endogenous incretin level, incretin activity and should restore glucose homeostasis in type II diabetic patients making it an attractive target for the development of new antidiabetic drugs. One of the interesting reported anti- DPP IV hits is Gemifloxacin which is used as a lead compound for the development of new DPP IV inhibitors. In the current work, design and synthesis of a series of N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives was carried out. The synthesized compounds were evaluated for their in vitro anti-DPP IV activity. Some of them have shown reasonable bioactivity, where the most active one 17 was found to have an IC50 of 33.5 μM.

scholarly journals Novel Ester and Acid Derivatives of the 1,5-Diarylpyrrole Scaffold as Anti-Inflammatory and Analgesic Agents. Synthesis and in Vitro and in Vivo Biological Evaluation

2010 ◽  
Vol 53 (2) ◽  
pp. 723-733 ◽  
Author(s):  
Mariangela Biava ◽  
Giulio C. Porretta ◽  
Giovanna Poce ◽  
Claudio Battilocchio ◽  
Fabrizio Manetti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Derivatives Of

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

scholarly journals Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus

MedChemComm ◽  
2017 ◽  
Vol 8 (5) ◽  
pp. 960-963 ◽  
Author(s):  
A. S. Sokolova ◽  
O. I. Yarovaya ◽  
M. D. Semenova ◽  
A. A. Shtro ◽  
I. R. Orshanskaya ◽  
...  
Keyword(s):  
Influenza A Virus ◽  
Influenza A ◽  
In Vitro Study ◽  
Vitro Study ◽  
Design And Synthesis ◽  
Heterocyclic Derivatives ◽  
Derivatives Of

Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (−)-borneol and (−)-isoborneol as potent inhibitors of the influenza A virus.

scholarly journals Synthesis and biological evaluation of heterocyclic 1,2,4-Triazole scaffolds as promising pharmacological agents

2020 ◽  
Author(s):  
Mukesh Kumari ◽  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Kalavathy Ramasamy ◽  
Siong Meng Lim ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Design And Synthesis ◽  
Hct 116

Abstract Background: Triazole is an important heterocyclic moiety that occupied a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms i.e. 1,2,4-triazole and 1,2,3-triazole and used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, antiurease , anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic, antimigrain agents.Methods: The structure of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (B. subtilis), Gram-negative (P. aeruginosa and E. coli) bacterial and fungal (C. albicans and A. niger) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-urease screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU and cisplatin as standards.Results, discussion and conclusion: The biological screening results reveal that the compounds T5 (MICBS, EC = 24.7µM, MICPA, CA = 12.3 µM) and T17 (MICAN = 27.1µM) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MICCipro = 18.1µM, MICAmo = 17.1µM) and fluconazole (MICFlu = 20.4µM), respectively. The antioxidant evaluation showed that compounds T2 (IC50 = 34.83 µg/ml) and T3 (IC50 = 34.38 µg/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC50 = 35.44 µg/ml). Compounds T3 (IC50 = 54.01µg/ml) was the most potent urease inhibitor amongst the synthesized compounds and compared to standard thiourea (IC50 = 54.25 µg/ml). The most potent anticancer activity showed by compounds T2 (IC50 = 3.84 μM) and T7 (IC50 = 3.25 μM) against HCT 116 cell lines as compared to standard 5-FU (IC50 = 25.36 μM).

scholarly journals Synthesis, Characterization and Biological Evaluation of Thiazolidinedione Derivative as Novel Antidiabetic Agents

2021 ◽  
pp. 123-133
Author(s):  
Shivkant Patel ◽  
Ashim Kumar Sen ◽  
Dillip Kumar Dash ◽  
Piyushkumar Sadhu ◽  
Mamta Kumari ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Peroxisome Proliferator ◽  
Peroxisome Proliferator Activated Receptor ◽  
Chemical Structures ◽  
Insulin Sensitizers ◽  
Diabetes Model ◽  
Glucose Synthesis ◽  
Sucrose Loading ◽  
Derivatives Of

Thiazolidinedione derivative have Antihyperglycemic activity, they are agonists for the peroxisome proliferator-activated receptor (PPAR), which controls glucose synthesis, transport, and utilization via regulating the transcription of insulin-responsive genes. A number of novel insulin sensitizers are currently being researched. Several of these are derivatives of Thiazolidinedione, but others have different chemical structures. In this work, we created some new Thiazolidinedione derivative based on structure–activity relationship as closely as feasible. The Thiazolidine-2,4-Dione derivatives were manually developed and synthesized using the proper synthetic techniques, then tested in vitro for antihyperglycemic action using the Sucrose loading model (SLM) and the Alloxan induced diabetes model (AIDM). The newly synthesized Thiazolidine-2,4-Dione derivative was characterized using infrared (IR) and proton (H) nuclear magnetic resonance. In this study we found that Compound M-4 has a lot of antihyperglycemic action, thus it's a good idea to think about using it as a lead material for the creation of anti-diabetic drugs.

scholarly journals Position-Selective Synthesis and Biological Evaluation of Four Isomeric A-Ring Amino Derivatives of the Alkaloid Luotonin A

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 716 ◽  
Author(s):  
Amra Ibric ◽  
Stefan Eckerstorfer ◽  
Martin Eder ◽  
Ivan Louko ◽  
Leopold Tunjic ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Human Tumor ◽  
Biological Evaluation ◽  
Transfer Hydrogenation ◽  
Amino Compound ◽  
M Cell ◽  
Luotonin A ◽  
Amino Derivatives ◽  
Derivatives Of

Following two orthogonal synthetic routes, a series of all four possible A-ring amino derivatives of the natural product Luotonin A (a known Topoisomerase I inhibitor) was synthesized. In both strategies, intramolecular cycloaddition reactions are the key step. The target compounds were obtained in good yields by mild catalytic transfer hydrogenation of the corresponding nitro precursors. In-vitro evaluation of the antiproliferative activity towards human tumor cell lines revealed the 4-amino compound (5b) to be the most effective agent, showing an interesting profile of cytotoxic activity. Among other effects, a significant G2/M cell cycle arrest was observed for this compound, suggesting that either Topoisomerase I is not the only biological target, or that some atypical mechanism is responsible for inhibition of this enzyme.

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