Quinoline alkaloid camptothecin (CPT) isolated in 1958 from Chinese tree Camptotheca acuminata is an important natural product serving as lead compound for designing many more active and clinically useful anticancer drugs, such as approved topotecan and irinotecan. All camptothecins exhibit a unique mechanism of action involving inhibition of topoisomerase I that leads to the interruption of cell division processes. Current efforts in CPT research focus on construction of better drugs, prodrugs and novel, mainly nano-sized forms of their administration. Important area of clinical work involves testing of multidrug regimens of CPTs with conjunction of other anticancer drugs. This often resulted in an improved activity toward malignancies. Besides anticancer activity camptothecins, they also display other bioactivities such as antiprotozoal, antifungal and insecticidal as well as inhibition of the SARS-CoV-2 virus. Insufficient natural supply of camptothecin led to significant improvement of camptothecins total synthesis and as well as to many attempts of their biotechnological production. Presented review covering over 300 references is intended to provide a complete but condensed overview on camptothecins, with emphasis on the newest work in the field.