Heterocyclic Molecular Targeted Drugs and Nanomedicines for Cancer: Recent Advances and Challenges

Abstract

Cancer is a top global public health concern. At present, molecular targeted therapy has emerged as one of the main therapies for cancer, with high efficacy and safety. The medical world continues to struggle with the development of efficient, extremely selective, and low-toxicity anticancer medications. Heterocyclic scaffolds based on the molecular structure of tumor therapeutic targets are widely used in anticancer drug design. In addition, a revolution in medicine has been brought on by the quick advancement of nanotechnology. Many nanomedicines have taken targeted cancer therapy to a new level. In this review, we highlight heterocyclic molecular-targeted drugs as well as heterocyclic-associated nanomedicines in cancer.

Discovery of Piperazin‐2‐yl‐pyrimidines as Anticancer Agents via Targeting JNK Signaling Pathway in Human MCF‐7 Breast Carcinoma

“…O-benzylated pyrimidine derivative (I) was treated with substituted piperazines (A) in presence of potassium iodide under basic conditions in DMF at 100 °C. After the completion of reaction, the crude product was extracted with ethyl acetate, concentrated under reduced pressure and purified through column chromatography using silica gel (60-120) and hexane:ethyl acetate as eluents, resulting in derivatives IA (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12).…”

“…[1,2] This versatility helps in overcoming the heterogeneity of cancer cells and their ability to develop resistance to specific drugs. [3,4] Numerous studies revealed that pyrimidine derivatives have a wide range of pharmacological action, including antibacterial, [5,6] anti-inflammatory, [7,8] antiviral, [9,10] and anticancer [11,12] activities. The most well-known drugs are based on pyrimidines such as 5-fluorouracil, pazopanib, and sorafenib agents, among others.…”

“…Heterocyclic drugs exhibit a wide range of mechanisms of action, allowing for multiple targets to be addressed simultaneously by inhibiting the activity of enzymes involved in signaling pathways, such as protein kinases, which regulate cell growth and survival [1,2] . This versatility helps in overcoming the heterogeneity of cancer cells and their ability to develop resistance to specific drugs [3,4] . Numerous studies revealed that pyrimidine derivatives have a wide range of pharmacological action, including antibacterial, [5,6] anti‐inflammatory, [7,8] antiviral, [9,10] and anticancer [11,12] activities.…”

Evaluation of Antitumor Activity of Xanthones Conjugated with Amino Acids

“…The use of scaffolds for drug discovery allows for the exploration of different chemicals, providing structural templates to optimize molecules with potential anticancer activity. For example, heterocyclic building blocks, like thiophenes, pirrole, or pyrazoles, demonstrated high efficiency in the treatment of different types of cancer, including metastatic models [3][4][5][6]. Over eighty-five percent of FDA-approved molecules contain heterocycles and have indicated potential benefits against a range of cancer treatments [7].…”

Synthesis of novel triazoles as anticancer agents targeting pJNK in human breast cancer cells

“…To effectively treat cancer, researchers seek innovative anticancer drugs with high selectivity and capacity to overcome drug resistance with minimum side effects. 3 BC is the most often diagnosed cancer among women, with a high mortality rate worldwide. 4 Various biological pathways, such as c-Jun-N-terminal kinase (JNK), play a vital role in BC regulation.…”