Tabriz University of Medical Sciences Advanced Pharmaceutical Bulletin 2228-5881 11 4 2021 09 19 Breast Cancer: a Global Concern, Diagnostic and Therapeutic Perspectives, Mechanistic Targets in Drug Development 580 594 10.34172/apb.2021.068 EN Gul-e-Saba Chaudhry https://orcid.org/0000-0002-4555-8572 Rehmat Jan Abdah Akim Muhammad Naveed Zafar Yeong Yik Sung Tengku Sifzizul Tengku Muhammad REVIEW 10.34172/apb.2021.068 2020 02 27 2020 10 14 Cancer is a complex multifactorial process, unchecked and abrupt division, and cell growth—conventional chemotherapy, along with radiotherapy, is used to treat breast cancer. Due to reduce efficacy and less survival rate, there is a particular need for the discovery of new active anticancer agents. Natural resources such as terrestrial/marine plants or organisms are a promising source for the generation of new therapeutics with improving efficacy. The screening of natural plant extracts and fractions, isolations of phytochemicals, and mechanistic study of those potential compounds play a remarkable role in the development of new therapeutic drugs with increased efficacy. Cancer is a multistage disease with complex signaling cascades. The initial study of screening whole extracts or fractions and later the isolation of secondary compounds and their mechanism of action study gives a clue of potential therapeutic agents for future drug development. The phytochemicals present in extracts/fractions produce remarkable effects due to synergistically targeting multiple signals. In this review, the molecular targets of extracts/ fractions and isolated compounds highlighted. The therapeutic agent's mechanistic targets in drug development focused involves; i) Induction of Apoptosis, ii) modulating cell cycle arrest, iii) Inhibition or suppression of invasion and metastasis and iv) various other pro-survival signaling pathways. The phytochemicals and their modified analogs identified as future potential candidates for anticancer chemotherapy.