Letters in Drug Design & Discovery - Volume 9, Issue 3, 2012

Cancer remains one of the leading causes of death in the world and as a result there is a pressing need for the development of novel and effective treatments. Cancer cells differ from their normal counterparts in a number of biochemical processes, particularly during the control of cell growth and division. Despite major breakthroughs in many areas of modern medicine over the past 100 years, the successful treatment of canc Read More

Castrate-resistant prostate cancer is associated with resistance to apoptotic-triggered cell death mediated by elevated expression of anti-apoptotic proteins. In the current study, the ability of three titanocene derivatives to induce apoptosis in PC-3 cells is investigated and compared to docetaxel as the standard therapy as a first step in the pre-clinical testing of these compounds against advanced prostate cancer. Apoptosis trigge Read More

A series of pyridylimidazolidinone linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates have been synthesized and evaluated for their DNA binding ability and cytotoxicity. These conjugates exhibited significant DNA binding ability and potent anticancer activity with GI50 values in the range of 0.2-3 μ M.

A new series of bisindole based sulfonates (4a-t) have been synthesized and evaluated for their anticancer activity against various human cancer cell lines. Some of these compounds exhibited good inhibitory activity against most of the cell lines tested. Interestingly all the compounds from the bisindole sulfonate series exhibited selective inhibition against MCF-7 cell line. Further these compounds have also been tested for their i Read More

A series of fourteen polysubstituted 7-chloro-4-quinolinylhydrazone derivatives (3a-n) has been synthesized and evaluated for their activity against four cancer cell lines. Among them, compounds 3a, 3c, 3h, 3i, 3j and 3n showed good cytotoxicity (with IC50 ranging from 0.7483 to 5.572 μg/mL). In general, we observed that the presence of methoxy groups on benzene ring plays an important role in the anticancer activity of this s Read More

A series of 14 N-acyl-hydrazones L-serine derivatives have been synthesized and evaluated for their in vitro antitumoral activities against four neoplastic cancer cells: HL-60 (leukemia), MDA-MB-435 (melanoma), HCT-8 (colon) and SF-295 (nervous system). Five compounds (3g, 3h, 3i, 3k and 3n) were considered active against at least two cancer cell lines, with more than 90% of growth inhibition. Compound 3h, with IC50 Read More

New advances in chemistry and biology have lead to the development of innovative approaches towards the treatment of deadly diseases like cancer. Particularly, glycochemistry and glycobiology have passed through a renaissance in the last two decades. This is apparent from the fact that the recent advances in the synthesis of tumor associated carbohydrate antigens (TACAs) have led to the development of various an Read More

A series of 3-[3-[4-(Substituted)-1-cyclicamine]propyl]thio-5-substituted[1,2,4]triazoles (8a-j) were synthesized with good yields starting from corresponding carboxylic acids. The cytotoxicity studies of these derivatives were studied against five different human cancer cell lines. Three compounds had shown good anticancer activity. The triazole derivatives, 8i and 8j were most potent particularly against U937 and HL-60 Read More

5-Substituted uracils were reported to be important core structure of diverse therapeutics. Herein, novel mixed ligand transition metal (Mn, Cu, Ni) complexes of 5-iodouracil (5Iu) with 8-hydroxyquinoline or 8HQ (1-3) and 5- nitrouracil (5Nu) with 8HQ (4-6) have been synthesized. The metal complexes 1-6 exert significant cytotoxicity against HepG2, A-549, HuCCA-1 and MOLT-3 cell lines. Particularly, the cytotoxicities of teste Read More

Quantitative relationships between structure of the selected 4-chloro-2-mercapto-5-methylbenzensulfonamide derivatives and their potential anticancer activity were studied. Molecular descriptors of studied compounds were obtained with the support of Dragon software after geometry optimization using HyperChem package. Theoretically calculated parameters were used to study the relationships between structure an Read More

The estrogen receptors (ERα and ERβ ), are ligand inducible nuclear receptors which play a key role in many cellular functions through specific gene expression regulation. The estrogen receptor is regarded as an attractive therapeutic target for hormone-dependent breast cancers. The antiestrogen drug tamoxifen is useful in the treatment of breast cancer. To develop new ER targeting agents as probes of estrogen rece Read More

The synthesis and structure-activity relationships (SAR) antitumor activities of monopyrazolic and bipyrazolic tripodal derivatives are reported here for the first time. The ten products were tested against three human cancer cell lines including breast (MDA-MB231), prostate (PC3) and colorectal (LoVo) cancers. In bipyrazolic series, most of them exhibited a moderate antitumor activity against three human cancer cell lines with a Read More

In the present study, some hydrazone derivatives were synthesized via the reaction of 3-cyclohexylpropionic acid hydrazide with various benzaldehydes. The chemical structures of the compounds were elucidated by spectroscopic techniques such as IR, 1H-NMR and FAB-MS and elemental analyses. The compounds were evaluated for their antiinflammatory and cytotoxic activities. Anti-inflammatory activity was d Read More

With an objective to evaluate the antibacterial activity of triazine derivatives, a series of 2,4,6-trisubstituted- 1,3,5-triazine were synthesized and characterized by FTIR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. The minimum inhibitory concentration (MIC) of the compounds that displayed favourable zone of inhibition was determined by broth microdilution method. Derivatives with morpholinyl sub Read More

A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calci Read More

Due to overwhelming generation of drug resistant microorganisms, there is an urgent need to develop novel chemotherapeutic agents. In continuation of our research on discovery of novel heterocyclic scaffolds from 1,3,5-triazine, present study deals with design and development of some novel di- and tri-substituted 1,3,5-triazine derivatives. The synthesis of title analogues were accomplished by SNAr reaction and su Read More

Flutamide (FLT) is the only presently recommended drug for monotherapy of benign prostatic hypertrophy. It is known for its poor solubility and slow dissolution. In this study nine different formulae of liquisolid systems (LS) were prepared using Polyethyleneglycol 400 as a liquid vehicle, Avicel® PH 102 and Aerosil 200 as the carrier and the coating material, respectively. Hydrophilic polymers (PVP, HPMC and PEG 2000) w Read More