Potential Anticancer Agents: Design, Synthesis of New Pyrido[1,2-a]benzimidazoles and Related Derivatives Linked to Alkylating Fragments
Journal Title: UNKNOWN - Year 2018, Vol 8, Issue 4
Abstract
The incentive of the present work has been primarily directed towards the design and synthesis of some novel pyrido[1,2-a]benzimidazoles with specific functionalities believed to have alkylation ability. This combination of pharmacological agents may enable synergistic anticancer effect. Nine compounds 5b, 13a, 13d, 13e, 14b, 14c, 15, 16, and 17 were selected by the National Cancer Institute (NCI), Bethseda, Maryland, USA to be evaluated for their in vitro antitumor activity. All the selected compounds were tested initially at a single dose (10 μM) in the full NCI 60 cell panel including leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast cancer cell lines. Majority of the test compounds exhibited moderate cytotoxic activity. The highest activity in all the investigated cancer cells was displayed by 14c against melanoma SK-MEL-5 cell line. This may be due to the impact of the lipophilic trifluoromethyl substitution on the biological activity profile.
Authors and Affiliations
Salma AZ Darwish, Rasha Y Elbayaa, Hayam MA Ashour, Mounir A Khalil, Elsayed AM Badawey
Keywords
Related Articles
- EP ID EP672577
- DOI -
- Views 56
- Downloads 0
Synthesis and Evaluation of Antiplasmodial Activities of Fluorinated 6-Amino- 2-Aryl-3H-Indolone-N-Oxides
A series of novel 6-amino-2-aryl-3H-indolone-N-oxides were synthesized at yields of up to 65% and characterized; one was further characterized using X-ray crystallographic analysis. Synthesized compounds were evaluated f...
Stem Cell in Lingual Epithelia and Papillae
In mammalian tongue, all the compartments of the lingual epithelium are turned over throughout adult life. There is a continual requirement for proliferation to replace cells lost by differentiation within each compartme...
Molecular Modeling Study of the Penetration Kinetic of Diverse Compounds through the Human Skin by Three-Dimensional Quantitative Structure Activity Relationship
The control of permeation is essential for the topical application of lotions, creams, and ointments, and the toxicological and risk assessment of materials from environmental and occupational hazards. This study develop...
Novel Chiral Chalcone Analogs that Induce M Phase Arrest and Apoptosis in HeLa Cells
We identified two chiral chalcone analogs CCL360 and CCL361 from the Chiba Chemical Library, which exhibit antiproliferative effects on human cancer cells. Flow cytometry analyses revealed that HeLa and Vero cells treate...
Taste Receptor Tas2r5 and Tas1r3 is Expressed in Sublingual Gland
Type 2 taste receptors (TAS2Rs), a large family of GPCRs, were first discovered in the gustatory system, and are co-expressed in a subset of taste receptor cells and detect bitter-tasting compounds. Type 1 taste receptor...