A new series of benzoxazole derivatives were designed and synthesised to have the main essential pharmacophoric features VEGFR-2 inhibitors. Cytotoxic activities evaluated for all against two human cancer cell lines, MCF-7 HepG2. Also, effect most cytotoxic on protein concentration was assessed by ELISA. Compounds

A thiazolidine-2,4-dione nucleus was molecularly hybridised with the effective antitumor moieties; 2-oxo-1,2-dihydroquinoline and 2-oxoindoline to obtain new hybrids potential activity against VEGFR-2. The cytotoxic effects of synthesised derivatives Caco-2, HepG-2, MDA-MB-231 cell lines were investigated. Compound 12a found be most potent candidate investigated IC50 values 2, 10, 40 µM, respectively. Furthermore, tested in vitro for their VEGFR-2 inhibitory showing strong inhibition....

A new series of pyrimidine-5-carbonitrile derivatives has been designed as ATP mimicking tyrosine kinase inhibitors the epidermal growth factor receptor (EGFR).

Guided by the structural optimization principle and promising anticancer effect of quinoxaline nucleus, a new series novel HDAC inhibitors were designed synthesized. The synthesized compounds to bear reported pharmacophoric features in addition an extra moiety occupy non-used vacant deep pocket receptor. newly prepared evaluated for their vitro anti-proliferative activities against HepG-2 HuH-7 liver cancer cell lines. tested showed both most active ten candidates ( 6 c , d f g k l 7 b 8 10...

New quinoline and isatin derivatives having the main characteristics of VEGFR-2 inhibitors was synthesised. The antiproliferative effects these compounds were estimated against A549, Caco-2, HepG2, MDA-MB-231. Compounds 13 14 showed comparable activities with doxorubicin Caco-2 cells. These strongly inhibited kinase activity. cytotoxic evaluated Vero Compound 7 highest value safety selectivity. Cell migration assay displayed ability compound to prevent healing abilities in cancer...

This work is one of our efforts to discover potent anticancer agents. We modified the most promising derivative previous concerned with development VEGFR-2 inhibitor candidates. Thirteen new compounds based on benzoxazole moiety were synthesized and evaluated against three human cancer cell lines, namely, breast (MCF-7), colorectal carcinoma (HCT116), hepatocellular (HepG2). The also kinase activity. biological testing fallouts showed that compound

We report herein, the design and synthesis of thiazolidine-2,4-diones derivatives as new inhibitors for VEGFR-2. The designed members were assessed their in vitro anticancer activity against four cancer cell lines; A549, Caco-2, HepG-2 MDA-MB-231. Compound 14a showed most potent effects lines (IC50 = 1.5 31.5 μM, respectively). Next, VEGFR-2 inhibitory activity, safety profiles selectivity indices examined all synthesized normal Vero line. (the safest member Caco-2 line) was further...

A new set of quinoline and isatine derivatives were synthesized as antiangiogenic VEGFR-2 inhibitors. On a biological level, the in vitro ability obtained candidates to inhibit was found be strong with IC50 values range 76.64-175.50 nM. To investigate cytotoxicity safety, all compounds tested against panel four cancer cell lines (A549, Caco2, HepG2 MDA) well two normal (Vero WI-38). Interestingly, compound 12 exhibited noticeable A549, Caco2 MDA 5.40, 0.58 0.94 µM, respectively. These...

In continuation of our previous work on the design and synthesis topoisomerase II (Topo II) inhibitors DNA intercalators, a new series quinoxaline derivatives were designed synthesized. The synthesized compounds evaluated for their cytotoxic activities against panel three cancer cell lines (Hep G-2, Hep-2, Caco-2). Compounds 18b, 19b, 23, 25b, 26 showed strong potencies all tested with IC50 values ranging from 0.26 ± 0.1 to 2.91 µM, comparable those doxorubicin (IC50 0.65 0.81 µM). most...

Abstract A new series of 1,2,4‐triazolo[4,3‐ c ]quinazoline derivatives was designed and synthesized as Topo II inhibitors DNA intercalators. The cytotoxic effect the members evaluated in vitro against a group cancer cell lines including HCT‐116, HepG‐2, MCF‐7. Compounds 14 , d e 15 b 18 19 exhibited highest activities with IC 50 values ranging from 5.22 to 24.24 µM. Furthermore, inhibitory intercalating affinities most promising candidates were possible mechanism for antiproliferative...

The Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) caused the “COVID-19” disease that has been declared by WHO as a global emergency. pandemic, which emerged in China and widespread all over world, no specific treatment till now. reported antiviral activities of isoflavonoids encouraged us to find out its silico anti-SARS-CoV-2 activity. In this work, molecular docking studies were carried investigate interaction fifty-nine against hACE2 viral Mpro. Several other including...

Herein, a new wave of bis([1, 2, 4]triazolo)[4,3-a:3',4'-c]quinoxaline derivatives have been successfully designed and synthesised. The synthesised were biologically investigated for their cytotoxic activities against HepG2 MCF-7. Also, the tested compounds further examined in vitro VEGFR-2 inhibitory activity. most promising derivative 23j was its apoptotic behaviour cell lines using flow cytometric western-plot analyses. Additional in-silico studies performed to predict how can bind...

There is an urgent need to design new anticancer agents that can prevent cancer cell proliferation even with minimal side effects. Accordingly, two series of 3-methylquinoxalin-2(1H)-one and 3-methylquinoxaline-2-thiol derivatives were designed act as VEGFR-2 inhibitors. The synthesised evaluated in vitro cytotoxic against human lines namely, HepG-2 MCF-7. Also, the assessed for their VEGFR-2inhibitory effect. most promising member 11e further investigated reach a valuable insight about its...

In this study, a set of novel benzoxazole derivatives were designed, synthesised, and biologically evaluated as potential VEGFR-2 inhibitors. Five compounds (12d, 12f, 12i, 12l, 13a) displayed high growth inhibitory activities against HepG2 MCF-7 cell lines further investigated for their activities. The most potent anti-proliferative member 12 l (IC50 = 10.50 μM 15.21 MCF-7, respectively) had the promising activity 97.38 nM). A biological evaluation revealed that compound 12l could arrest...

Increase in the number of infections caused by pathogenic microbes cancer patients has prompted searcher to invest development agents having dual anticancer and antimicrobial properties. The present study is concerned with synthesis screening for activity a series 5-hydrazinyl-2-(2-(1-(thien-2-yl)ethylidene)hydrazinyl)thiazole derivatives. structure elucidation synthesized hydrazinyl thiazole derivatives was illustrated spectroscopic elemental analysis. All newly compounds 5a-p were...

Background: VEGFR-2 is one of the most effective targets in cancer treatment. Aim: The design and semi-synthesis new theobromine derivatives as potential inhibitors. Methods: In vitro silico evaluation synthesized compounds. Results: Compound 5b demonstrated excellent antiproliferative inhibitory effects with significant apoptotic activity. It modulated immune response by increasing IL-2 reducing TNF-α levels. Docking molecular dynamics simulations revealed compound’s binding affinity...

Different 2,4-thiazolidinedione-tethered coumarins 5a-b, 10a-n and 11a-d were synthesised evaluated for their inhibitory action against the cancer-associated hCAs IX XII, as well physiologically dominant I II to explore selectivity. Un-substituted phenyl-bearing 10a, 10 h, 2-thienyl/furyl-bearing 11a-c exhibited best hCA (KIs between 0.48 0.93 µM) XII 0.44 1.1 actions. Interestingly, none of had any effect on off-target isoforms. The sub-micromolar compounds from biochemical assay, h 11a-c,...

Cancer is still a dangerous disease with high mortality rate all over the world. In our attempt to develop potential anticancer candidates, new quinazoline and phthalazine based compounds were designed synthesized. The derivatives built in line pharmacophoric features of thalidomide. as well thalidomide examined against three cancer cell lines, namely: hepatocellular carcinoma (HepG-2), breast (MCF-7) prostate (PC3). Then effects on expression levels caspase-8, VEGF, NF-κB P65, TNF-α HepG-2...

Novel thalidomide analogs as anticancer immunomodulatory agents.

In this study, novel VEGFR-2-targeting thiazolidine-2,4-dione derivatives with potential anticancer properties were designed and synthesized. The ability of the to inhibit VEGFR-2 stop growth three different cancer cell types (HT-29, A-549, HCT-116) was examined

In this study, a series of seven novel 2,4-dioxothiazolidine derivatives with potential anticancer and VEGFR-2 inhibiting abilities were designed synthesized as inhibitors. The compounds tested in vitro for their to inhibit the growth HepG2 MCF-7 cancer cell lines. Among tested, compound 22 (IC50 = 0.079 μM) demonstrated highest anti-VEGFR-2 efficacy. Furthermore, it significant anti-proliferative activities against 2.04 ± 0.06 1.21 0.04 M). Additionally, also increased total apoptotic rate...