Increased risks of peripheral toxicity and undesired adverse effects associated with chemotherapeutic agents are the major medical hurdles in cancer treatment that worsen the quality of life of cancer patients. Although several novel and target-specific anticancer agents have been discovered in the recent past, none of them have proved to be effective in the management of metastatic tumor. Therefore, there is a continuous effort for the discovery of safer and effective cancer chemotherapeutic agent. Adenosine receptors have been identified as an important target to combat cancer because of their inherent role in the antitumor process. The antitumor property of the adenosine receptor is primarily attributed to their inherited immune response against the tumors. These findings have opened a new chapter in the anticancer drug discovery through adenosine receptor-mediated immunomodulation. This review broadly outlines the biological mechanism of adenosine receptors in mediating the selective cytotoxicity as well as the discovery of various classes of adenosine receptor modulators in the effective management of solid tumors.

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The clinical use of anthraquinone antibiotics such as doxorubicin in cancer chemotherapy is limited due to their toxic cardiomyopathy effects. The conjugation of anthraquinones with fatty acids is known to enhance bioactivity by increasing lipophilicity and facilitating cell membrane permeation. Short‐chain saturated fatty acids such as capric, caprylic, caproic acids, and lauric acids are known for their inherent anticancer properties on human colorectal cancer cells. In this study, 2‐hydroxyanthraquinone and saturated fatty acid esters were synthesized and evaluated against human colon cancer cell line HT‐29 and Colo‐205, breast cancer cell lines MDA‐MB‐231 and MCF‐7, and leukemia cell line K‐562 for their in vitro anticancer properties using a sulforhodamine B (SRB) assay. The anthraquinone‐saturated fatty acid conjugates produced excellent activity against human colon and breast cancer cell lines. The octanoic acid and hexanoic acid derivatives of 2‐hydroxy anthraquinone showed excellent anticancer activity with GI50 values of 0.2 nM and 1.0 nM against human colon cancer cell line Colo‐205 and the human breast cancer cell line MCF‐7, respectively, and emerged as the most active compounds. Furthermore, the in vitro cytotoxicity study against peripheral blood mononuclear cells showed that these derivatives are non‐toxic in nature.