Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 16, Issue 2, 2016

Acetogenins (ACG) are naturally occurring compounds that are chemically one of the least investigated families. In the review, we have provided a comprehensive listing of 133 of these compounds for which anti-tumor activity has been documented within the literature. We have compiled and studied their chemical structure, in-vitro as well as in-vivo anticancer biological activity. We observed that the relative potency of acetog Read More

Breast cancer (BC) is the second most common cause of cancer-related deaths in women throughout the world. Multiple drugs have been approved by US-FDA for breast related malignancies. Frequent emergence of resistances creates the severe need of newer moieties that are free from such problems. Drugs targeting breast cancer have been observed to be based on the multiple mechanisms of action, and various Read More

p53 protein is a prominent tumor suppressor to induce cell cycle arrest, apoptosis and senescence, which attracts significant interest to cancer treatment. Therefore, it would be particularly important to restore the wild–type p53 that retains latent functions in the approximately 50% of tumors. MDM2 (murine double minute 2), the principal cellular antagonist of p53, has long been believed to suppress p53 activity throug Read More

ROS have vital roles in cellular signaling and homeostasis. At low concentration, ROS promotes cancer cell survival by the activation of growth factors and MAP-kinases (MAPKs) that further activates cell cycle progression. At high concentration, ROS produces oxidative stress that activates programmed cell death or apoptosis. However, this fine distinction of ROS action either as a growth promoter or pro-apoptotic agent de Read More

Chalcones comprise a characteristic framework of 1, 3-diaryl-2-propen-1-one. They have been heralded as promising anti cancer drugs and have received much attention in the field of cancer research and drug development. The cytotoxicity of these potent pharmacophores is attributable to a wide spectrum of biological activities like anti inflammatory, anti proliferative, anti fungal, etc. These anti tumor activities are effectuat Read More

Treatment of brain tumour is a major challenge. This is mainly because of the limited bioavailability of chemotherapeutics in the brain. The major hurdle for brain availability of anticancer agents is the blood brain barrier (BBB). BBB is supposed to protect the brain and maintain homeostasis. It allows vital nutrient for normal brain function and effluxes out foreign toxic substance. Advance in knowledge of bidirectional movement Read More

DNA interstrand crosslinks (ICLs) can be induced by numerous endogenous and exogenous chemical agents with the capacity of covalently binding to two base sites in the two strands of the DNA duplex. A series of normal DNA metabolism processes are affected by ICLs. For example, DNA replication and transcription are interfered during cell division, which is fatal to cell survival. In cancer cells, the induction of ICLs is a sig Read More

MicroRNAs (miRNAs) have a major role in cancer pathogenesis, cells growth and apoptosis. We studied the dysregulation of miRNAs after the induction of apoptosis by 4 μM dose of ATO in glioblastoma cell line, U87. The anticancer effect of ATO was verified using MTT, BrdU cell proliferation assay and flow cytometric analysis. Differential expressions of 88 cancer-related miRNAs were analyzed by real-time revers Read More

Treatment of non melanoma skin cancer and its precancerous skin lesions is associated with severe topical and systemic toxicity. So, it has become necessary to develop an efficient novel delivery system with less side effects and better patient compliance. Topical w/o microemulsion of 5-FU were prepared using sorbitan monooleate (Span 80), sorbitan trioleate (Span 85), polysorbate 80 (Tween 80), isopropyl alcohol (IPA) with Read More

A series of novel 5-(substituted phenyl)-3-[(substituted phenylamino)methyl]-3H-[1,3,4]oxadiazole-2- thione derivatives were prepared and their in vitro cytotoxicity was evaluated against a panel of three cancer cell lines, namely, hepatocarcinoma HepG2, breast adenocarcinoma MCF-7, and leukemia HL-60 cells, using the widely accepted MTT assay. In general, the synthesized compounds displayed weak to moderate cytotoxi Read More