Letters in Drug Design & Discovery - Volume 8, Issue 10, 2011

The combined activity of MGBG (metylglyoxal-bis(guanylhydrazone)) with either cisplatin or carboplatin was investigated, towards the human breast cancer cell line MCF-7. While a dose- and time-dependent cytotoxic activity was already observed for MGBG alone, a synergistic and non-reversible effect was verified upon co-administration with these Pt-based drugs. Furthermore, toxicity against non-neoplastic cells was shown to be Read More

Platinum-based chemotherapeutic agents such as carboplatin, cisplatin, and oxaliplatin are used to treat a broad range of malignant diseases. Their efficacies in most cancers are limited by the development of resistance. There are multiple factors that contribute to platinum resistance but alterations of DNA repair processes have been known for some time to be important in mediating resistance. The two anticancer drug c Read More

Two C5-substituted licofelone derivatives were developed and investigated for cytotoxicity against mammary (MCF-7 and MDA-MB 231) as well as colon carcinoma (HT-29) cancer cells. Both compounds were at least 2-fold more active than 5-fluorouracil (5-FU) and licofelone against mammary carcinoma cells. At HT-29 cells, they were less active, but nevertheless distinctly as active as 5-FU and still 2-fold more active than licofel Read More

A quantitative structure-activity relationship (QSAR) study has been made on a novel series of substituted 3-[3-(aminopropyl)-4,5,6,7-tetrahydro-1H-indol-2-ylmethylene]-1,3-dihydro-indole-2-ones as potent inhibitors of the non-receptor Src tyrosine kinase. The activity is found to be significantly correlated with calculated hydrophobicity and molar refractivity of the molecule. The correlation obtained suggests that the activity of t Read More

The growth and metastasis of solid tumors are dependent on angiogenesis. The vascular endothelial growth factor (VEGF) is of particular interest since it is essential for angiogenesis. The development of novel inhibitors of VEGF receptor type 2 (VEGFR-2) is important. Quantitative structure-activity relationship (QSAR) studies were performed to understand the structural factors affecting inhibitory potency of 4-aryl-5-cyano-2- Read More

Estrogens are responsible for the growth of hormone-dependant breast cancer. Regulation of estrogen biosynthesis is considered as a potential therapeutic strategy for the control of breast cancer. The enzyme aromatase catalyzes conversion of androgens into estrogens in the last step of estrogen biosynthesis. Inhibition of aromatase is adopted as an efficient approach for the prevention and treatment of breast cancer. M Read More

SSH-BM-I is a new synthetic compound that is synthesized from Bromomelatonin by using a newly developed synthetic method. Recently, our group demonstrated that SST-VED-I-1, which has a similar chemical structure to SSHBM- I, inhibits starvation-induced apoptosis in osteoblasts. However, the effects of SSH-BM-I on apoptosis in osteoblasts have not yet been examined. Therefore, this study examined the effects of this comp Read More

A series of new cinnamide dimers was synthesized (5a-6a) and evaluated for their antimicrobial and antifungal activity. All the compounds investigated have shown significant antimicrobial activity against gram-positive and gram-negative bacterial strains, as well as few fungal strains. The compounds having withdrawing group exhibited significant biological activity than their precursors. Moreover all the compounds con Read More

A series of novel 4” -O-2-arylbenzimidazolyl derivatives of clarithromycin were synthesized and evaluated. These 4” -O-2-arylbenzimidazolyl derivatives demonstrated excellent activity against erythromycin-susceptible strains and showed remarkably improved activity against erythromycin-resistant strains compared with the references. In particular, compound 7c, which possesses the terminal 2-(2-methoxyph Read More

New anacardic acid derivatives (5a -5s) were prepared from commercially available anacardic acid and tested for Gram positive and Gram negative bacteria. Most compounds were found to be active compared to ampicillin drug.

Resistance to commercially available antimicrobials is increasing at alarming rate therefore there is an urgent need of new antimicrobial compounds and materials with novel modes of action to tackle the problem of resistance in pathogenic gram positive and gram negative bacteria. The current study involves the design and synthesis of new molecular structures which should not resemble the basic molecular structur Read More

A series of novel 2-methyl-3-(2-(piperazin-1-yl)ethyl)-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one sulfonamide and carboxamide derivatives were synthesized in good yield. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesised compounds were screened for their in vitro antimicrobial activity by agar well diffusion and micro dilution method against standard strai Read More

Estrogen, the key regulator of the cellular process involved in the development and maintenance of reproductive functions, mediates its action through estrogen receptor binding, and initiating a series of cellular pathway producing estrogen-induced responses. At higher dose, it can effectively act as contraceptive but associates with risk factors. Considering the long-term benefit-to-risk ratio of estrogen analogs as or Read More

1,2,4-Triazoles, pyrazoles and semicarbazides possessing heterocyclic ring 1-14 were synthesized as compounds with interesting pharmacological profiles. All were investigated in vitro for their antioxidant activity. Some compounds showed significant effect in the above assay. The most promising was a group of pyrazolone. The effect was dependent mainly on the substituent on the amide group. It was found that compo Read More

In order to understand the molecular mechanism of Tongguan capsule (TGC), a Traditional Chinese Medicine (TCM) for coronary heart disease (CHD), computational approaches of pharmacodynamic modeling were introduced to predict the interaction between drugs and targets about cardiovascular system. Firstly, we employed a molecular docking protocol to study the interaction of natural compounds from TGC and Read More